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| Product | Description | |
|---|---|---|
| Mutant EGFR inhibitor | Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1. It inhibits EGFRL858R, EGFRExon 19 deletionand EGFRT790M. Group: Pharmaceutical. Alternative Names: MDK3627; MDK 3627; MDK-3627; Mutant EGFR inhibitor. CAS No. 1421373-62-7. Pack Sizes: 5 mg. Product ID: B0084-463231. Molecular formula: C27H30ClN7O2. Mole weight: 520.03. Custom synthesis is available. Send your inquiries for more information. |  London |
| AEE-788 | AEE-788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and vascular endothelial growth factor receptor 2 (VEGF2), resulting in receptor inhibition, the inhibition of cellular proliferation, and induction of tumor cell and tumor-associated endothelial cell apoptosis. Group: Pharmaceutical. Alternative Names: AEE 788; AEE788; 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine. CAS No. 497839-62-0. Pack Sizes: 10 mg. Product ID: B0084-258485. Molecular formula: C27H32N6. Mole weight: 440.595. Custom synthesis is available. Send your inquiries for more information. | London |
| AG-1557 | AG-1557 is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Group: Pharmaceutical. Alternative Names: AG-1557; AG 1557; AG1557; N-(3-Iodophenyl)-6,7-dimethoxyquinazolin-4-amine. CAS No. 189290-58-2. Pack Sizes: 50 mg. Product ID: B0084-284805. Molecular formula: C16H14IN3O2. Mole weight: 407.211. Custom synthesis is available. Send your inquiries for more information. | London |
| AG-490 | Tyrphostin AG490 is a JAK-2 specific inhibitor, which inhibits phosphorylation of EGFR and signal transducer and activator of transcription 3 [STAT-3], and subsequently reduce invasion and adhesion potential of malignant cells. Uses: Antineoplastic agents. Group: Pharmaceutical. Alternative Names: Tyrphostin AG 490; AG-490; AG490. CAS No. 133550-30-8. Pack Sizes: 25 mg. Product ID: B0084-164022. Molecular formula: C17H14N2O3. Mole weight: 294.31. Custom synthesis is available. Send your inquiries for more information. | London |
| AG-879 | AG-879, a tyrphostin compound, is a dual EGFR/HER2 inhibitor that was administered together with androgen withdrawal therapy. It inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM). Group: Pharmaceutical. Alternative Names: α-Cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide. CAS No. 148741-30-4. Pack Sizes: 20 mg. Product ID: B0084-195953. Molecular formula: C18H24N2OS. Mole weight: 316.5. Custom synthesis is available. Send your inquiries for more information. | London |
| AV-412 | AV-412 is a second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may suppress tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. This agent may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization. Group: Pharmaceutical. Alternative Names: AV 412; AV412; N-[4-(3-chloro-4-fluoroanilino)-7-[3-methyl-3-(4-methylpiperazin-1-yl)but-1-ynyl]quinazolin-6-yl]prop-2-enamide. CAS No. 451492-95-8. Pack Sizes: 20 mg. Product ID: B0084-324573. Molecular formula: C27H28ClFN6O. Mole weight: 507.01. Custom synthesis is available. Send your inquiries for more information. | London |
| AZ5104 | AZ5104 is a potent EGFR inhibitor and a derivative of AZD 9291. AZ5104 exhibits reduced selectivity against wild-type EGFR but five-fold potentcy compared to AZD 9291. Group: Pharmaceutical. Alternative Names: AZ-5104; AZ 5104; N-[2-[2-(dimethylamino)ethyl-methylamino]-5-[[4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-4-methoxyphenyl]prop-2-enamide. CAS No. 1421373-98-9. Pack Sizes: 25 mg. Product ID: B0084-470856. Molecular formula: C27H31N7O2. Mole weight: 485.592. Custom synthesis is available. Send your inquiries for more information. | London |
| AZD3759 | AZD3759 is a n orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. Group: Pharmaceutical. Alternative Names: AZD3759; AZD-3759; AZD 3759. CAS No. 1626387-80-1. Pack Sizes: 1 g. Product ID: B0084-470884. Molecular formula: C22H23ClFN5O3. Mole weight: 459.91. Custom synthesis is available. Send your inquiries for more information. | London |
| AZD-9291 | AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 μM, respectively). Uses: For research used only. Group: Pharmaceutical. Alternative Names: Mereletinib; AZD9291; AZD 9291; Osimertinib. CAS No. 1421373-65-0. Pack Sizes: 2.5 g. Product ID: B0084-462147. Molecular formula: C28H33N7O2. Mole weight: 499.61. Custom synthesis is available. Send your inquiries for more information. | London |
| AZD9291DA | AZD9291-DA is a des acryl analogue of AZD9291, which is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. Uses: For research used only. Group: Pharmaceutical. Alternative Names: AZD9291-Des acryl analogue; AZD9291 Des acryl precursor; Mutated EGFR-IN-1; N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine; N1-(2-dimethylaminoethyl)-5-methoxy-N1-methyl-N4-[4-(1-methylindol-3-yl)pyrimidin-2-yl]benzene-1,2,4-triamine; SCHEMBL14660679. CAS No. 1421372-66-8. Pack Sizes: 1 g. Product ID: B0084-462681. Molecular formula: C25H31N7O. Mole weight: 445.571. Custom synthesis is available. Send your inquiries for more information. | London |
| AZD-9291 mesylate | AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. Group: Pharmaceutical. Alternative Names: Mereletinib mesylate; EGFR inhibitor; AZD9291 mesylate; AZD 9291 mesylate. CAS No. 1421373-66-1. Pack Sizes: 100 mg. Product ID: B0084-463232. Molecular formula: C29H37N7O5S. Mole weight: 595.71. Custom synthesis is available. Send your inquiries for more information. | London |
| Brigatinib | Brigatinib, also known as AP-26113, is an orally active, potent and selective dual ALK/EGFR inhibitor. AP26113 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK; IC50 < 100 nM in Ba/F3 cells). AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. It blocks ALK activity and reduces growth in neuroblastoma cells, mouse xenograft, and Drosophila model systems harboring constitutively active ALK variants. Group: Pharmaceutical. Alternative Names: AP26113. CAS No. 1197953-54-0. Pack Sizes: 1 g. Product ID: B0084-470820. Molecular formula: C29H39ClN7O2P. Mole weight: 584.1. Custom synthesis is available. Send your inquiries for more information. | London |
| Chrysophanol | Chrysophanic acid (Chrysophanol) is a natural anthraquinone with anticancer activity in EGFR-overexpressing SNU-C5 human colon cancer cells. Chrysophanic acid preferentially blocked proliferation in SNU-C5 cells but not in other cell lines (HT7, HT29, KM12C, SW480, HCT116 and SNU-C4) with low levels of EGFR expression. Chrysophanic acid treatment in SNU-C5 cells inhibited EGF-induced phosphorylation of EGFR and suppressed activation of downstream signaling molecules, such as AKT, extracellular signal-regulated kinase (ERK) and the mammalian target of rapamycin (mTOR)/ribosomal protein S6 kinase (p70S6K). Chrysophanic acid (80 and 120 μm) significantly blocked cell proliferation when combined with the mTOR inhibitor, rapamycin. These findings offer the first evidence of anticancer activity for chrysophanic acid via EGFR/mTOR mediated signaling transduction pathway. Chrysophanol is a natural compound found in the roots and rhizomes of Rheum palmatum L. It can be used in cosmetics material. Uses: Anti-inflammatory. Group: Pharmaceutical. Alternative Names: 1,8-dihydroxy-3-methylanthracene-9,10-dione. CAS No. 481-74-3. Pack Sizes: 1 g. Product ID: NP0901. Molecular formula: C15H10O4. Mole weight: 254.24. Custom synthesis is available. Send your inquiries for more information. | London |
| CL-387785 | CL-387785, also known as EKI-785, is an irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM). CL-387785 covalently bound to EGF-R. It also specifically inhibited kinase activity of the protein (IC50 = 370+/-120 pM), blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2, and profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80 mg/kg/day for 10 days, daily). CL-387,785 is useful for studying the interaction of small molecules with EGF-R and may have clinical utility. Uses: Protein kinase inhibitors. Group: Pharmaceutical. Alternative Names: CL-387785; CL 387785; CL-387,785; CL387785; EKI-785; EKI 785; EKI785. CAS No. 194423-06-8. Pack Sizes: 50 mg. Product ID: B0084-458793. Molecular formula: C18H13BrN4O. Mole weight: 381.233. Custom synthesis is available. Send your inquiries for more information. | London |
| CNX-2006 | CNX-2006 is a potent and mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. Group: Pharmaceutical. Alternative Names: CNX2006; CNX 2006; N-[3-[[2-[4-[[1-(2-fluoroethyl)azetidin-3-yl]amino]-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide. CAS No. 1375465-09-0. Pack Sizes: 10 mg. Product ID: B0084-462328. Molecular formula: C26H27F4N7O2. Mole weight: 545.543. Custom synthesis is available. Send your inquiries for more information. | London |
| Dacomitinib | Dacomitinib, aslo known as PF-299 and PF-00299804; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types. Group: Pharmaceutical. Alternative Names: dacomitinib; PF-00299804; PF00299804; PF 00299804; PF299804; PF-299804; PF 299804; PF-299; PF 299; PF299. CAS No. 1110813-31-4. Pack Sizes: 250 mg. Product ID: B0084-452473. Molecular formula: C24H25ClFN5O2. Mole weight: 469.945. Custom synthesis is available. Send your inquiries for more information. | London |
| Desmethyl Erlotinib | A metabolite of Erlotinib. Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity. Group: Pharmaceutical. Alternative Names: 2-[[4-[(3-Ethynylphenyl)amino]-7-(2-methoxyethoxy)-6-quinazolinyl]oxy]ethanol. CAS No. 183321-86-0. Pack Sizes: 5 mg. Product ID: B2694-263407. Molecular formula: C21H21N3O4. Mole weight: 379.42. Custom synthesis is available. Send your inquiries for more information. | London |
| DM1-SMCC | DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate, as a potent EGFR inhibitor and it overcomes resistant to EGFR. Uses: This active molecular is dm1 with a linker smcc that can react with antibody to make antibody drug conjugate. Group: Pharmaceutical. Alternative Names: 2,5-dioxopyrrolidin-1-yl 4-((3-((3-(((2S)-1-(((14S,16S,33S,2R,4R,10E,12Z,14R)-86-chloro-14-hydroxy-85,14-dimethoxy-33,2,7,10-tetramethyl-12,6-dioxo-7-aza-1(6,4)-oxazinana-3(2,3)-oxirana-8(1,3)-benzenacyclotetradecaphane-10,12-dien-4-yl)oxy)-1-oxopropan-2-yl)(methyl)amino)-3-oxopropyl)thio)-2,5-dioxopyrrolidin-1-yl)methyl)cyclohexane-1-carboxylate; DM1 SMCC; SMCC-DM1. CAS No. 1228105-51-8. Pack Sizes: 10 mg. Product ID: BBF-04656. Molecular formula: C51H66ClN5O16S. Mole weight: 1072.62. Custom synthesis is available. Send your inquiries for more information. | London |
| DM1-SPP | DM1 with a reactive linker SPP, which can react with antibody to make antibody drug conjugate, as a potent EGFR inhibitor and it overcomes resistant to EGFR. Group: Pharmaceutical. Alternative Names: N2'-deacetyl-N2'-[3-[[4-[(2,?5-dioxo-1-pyrrolidinyl)?oxy]?-1-methyl-4-oxobutyl]?dithio]?-1-oxopropyl]?-Maytansine; DM1 SPP. CAS No. 452072-20-7. Pack Sizes: 5 mg. Product ID: BADC-00010. Molecular formula: C44H59ClN4O14S2. Mole weight: 967.54. Custom synthesis is available. Send your inquiries for more information. | London |
| EAI045 | EAI045 is an allosteric, non-ATP competitive inhibitor of mutant EGFR. In vitro studies proved that EAI045 is active and selective for T790M- harboring EGFR mutants that are in a monomer state. In vivo the combination of EAI045 and cetuximab caused a marked tumor shrinkage in a mouse model carrying the EGFR mutant with L858R/T790M/C797S. Therefore, EAI045 is the first allosteric inhibitor that targets T790M and C797S EGFR mutants but it is effective only in combination with cetuximab. Group: Pharmaceutical. Alternative Names: 2-(5-fluoro-2-hydroxyphenyl)-2-(3-oxo-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide; 2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide; EAI045; EAI 045; EAI-045. CAS No. 1942114-09-1. Pack Sizes: 50 mg. Product ID: B0084-475458. Molecular formula: C19H14FN3O3S. Mole weight: 383.397. Custom synthesis is available. Send your inquiries for more information. | London |
| EGF816 | EGF816, also called as Nazartinib, a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M resistance mutation while sparing wild-type EGFR. in vivo: demonstrated strong tumor regressions in several EGFR activating and resistant tumor m. Group: Pharmaceutical. Alternative Names: EGF816; EGF-816; EGF 816; NVS-816; NVS 816; NVS816; Nazartinib; N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamideEGF816UNII-KE7K32EME8KE7K32EME8EGF-8161508250-71-2GTPL9204SCHEMBL16767232SCHEMBL16767240EGF 816compound 47 [PMID: 27433829]. CAS No. 1508250-71-2. Pack Sizes: 10 mg. Product ID: B0084-474599. Molecular formula: C26H31ClN6O2. Mole weight: 495.02. Custom synthesis is available. Send your inquiries for more information. | London |
| Erlotinib | Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib has been indicated for non-small cell lung cancer (NSCLC) and pancreatic cancer therapy. Group: Pharmaceutical. Alternative Names: CP358774; CP 358774; CP-358774; NSC 718781; NSC718781; NSC-718781. CAS No. 183321-74-6. Pack Sizes: 10 g. Product ID: NP3245. Molecular formula: C22H23N3O4. Mole weight: 393.44. Custom synthesis is available. Send your inquiries for more information. | London |
| Erlotinib-3-vinyl Hydrochloride | A metabolite of Erlotinib. Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity. Group: Pharmaceutical. Alternative Names: 6,7-Bis(2-methoxyethoxy)-N-(3-vinylphenyl)quinazolin-4-amine hydrochloride; 4-Quinazolinamine, N-(3-ethenylphenyl)-6,7-bis(2-methoxyethoxy)-, hydrochloride (1:1). CAS No. 1624294-38-7. Pack Sizes: 25 mg. Product ID: B1370-173396. Molecular formula: C22H26ClN3O4. Mole weight: 431.91. Custom synthesis is available. Send your inquiries for more information. | London |
| Erlotinib-[d6] Hydrochloride | Erlotinib-[d6] Hydrochloride is the labelled analogue of Erlotinib. Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity. Erlotinib is a medication used to treat non-small cell lung cancer and pancreatic cancer. Group: Pharmaceutical. Alternative Names: N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy-d3)-4-quinazolinamine Hydrochloride; 6,7-Bis(2-methoxyethoxy-d3)-4-(3-ethynylanilino)quinazoline Hydrochloride; [6,7-Bis(2-methoxyethoxy-d3)quinazolin-4-yl]-(3-ethynylphenyl)amine Hydrochloride; Erlotinib D6 Hydrochloride. CAS No. 1189953-78-3. Pack Sizes: 5 mg. Product ID: BLP-006076. Molecular formula: C22H18D6ClN3O4. Mole weight: 435.93. Custom synthesis is available. Send your inquiries for more information. | London |
| Erlotinib Impurity 8 | A metabolite of Erlotinib. Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity. Group: Pharmaceutical. Alternative Names: N-(3-Desethynylphenyl)-N-(3-bromophenyl) Erlotinib; N-(3-bromophenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine. CAS No. 328528-74-1. Pack Sizes: 25 mg. Product ID: B2694-471125. Molecular formula: C20H22BrN3O4. Mole weight: 448.32. Custom synthesis is available. Send your inquiries for more information. | London |
| Erlotinib O-Desmethyl Metabolite Isomer (M14) HCl | OSI-420 (CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells. Uses: For research used only. Group: Pharmaceutical. Alternative Names: OSI420; OSI-420; OSI 420; CP473420; CP-473420; CP 473420; Desmethyl Erlotinib. CAS No. 183320-51-6. Pack Sizes: 10 mg. Product ID: B0084-286627. Molecular formula: C21H22ClN3O4. Mole weight: 415.874. Custom synthesis is available. Send your inquiries for more information. | London |
| Icotinib | Icotinib Hydrochloride (BPI-2009H), or Icotinib, is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Group: Pharmaceutical. Alternative Names: BPI-2009H. CAS No. 610798-31-7. Pack Sizes: 300 mg. Product ID: B0084-459334. Molecular formula: C22H21N3O4. Mole weight: 391.42. Custom synthesis is available. Send your inquiries for more information. | London |
| Icotinib hydrochloride | Icotinib Hydrochloride is a quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), which is upregulated in a variety of cancer cell types. Icotinib supresses the cancer cell proliferation via EGFR tyrosine kinase inhibition. Group: Pharmaceutical. Alternative Names: Icotinib HCl; BPI-2009; BPI 2009; BPI2009. CAS No. 1204313-51-8. Pack Sizes: 300 mg. Product ID: BBF-04036. Molecular formula: C22H22ClN3O4. Mole weight: 427.88. Custom synthesis is available. Send your inquiries for more information. | London |
| JNJ-26483327 | JNJ-26483327 is an orally bioavailable, small-molecule, multitargeted reversible tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3). By inhibiting several different signaling molecules that play crucial roles at various stages in tumorigenesis, this agent may inhibit tumor growth, invasion, migration and metastasis. In addition, JNJ-26483327 crosses the blood-brain barrier (BBB). Group: Pharmaceutical. Alternative Names: JNJ-26483327; JNJ 26483327; JNJ26483327. CAS No. 807640-87-5. Pack Sizes: 10 mg. Product ID: B0084-462547. Molecular formula: C22H25BrN4O2. Mole weight: 457.372. Custom synthesis is available. Send your inquiries for more information. | London |
| Lapatinib | Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively. Uses: Antineoplastic agents; protein kinase inhibitors. Group: Pharmaceutical. Alternative Names: GW-572016; GSK-572016; GSK 572016. CAS No. 231277-92-2. Pack Sizes: 1 g. Product ID: NP3214. Molecular formula: C29H26ClFN4O4S. Mole weight: 581.06. Custom synthesis is available. Send your inquiries for more information. | London |
| Methyl 2,5-dihydroxycinnamate | Methyl 2,5-dihydroxycinnamate, a stable analog of erbstatin, is a stable, potent inhibitor of EGFR kinase activity. It is described to be four-times more stable than erbstatin in calf serum2. It was shown to delay the S-phase induction by epidermal growth factor in quiescent normal rat kidney cells, without affecting the total amount of DNA synthesis. Group: Pharmaceutical. Alternative Names: Methyl 2,5-dihydoxycinnamate; 3-(2,5-dihydroxyphenyl)-2-propenoic acid, methyl ester; Erbstatin Analog. CAS No. 63177-57-1. Pack Sizes: 100 mg. Product ID: B0084-012976. Molecular formula: C10H10O4. Mole weight: 194.19. Custom synthesis is available. Send your inquiries for more information. | London |
| Mubritinib | Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinical trials (may be discontinued since 2008). Mubritinib(TAK 165) is a potent EGFR, HER2 and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 μM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. Mubritinib(TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib(TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo. Group: Pharmaceutical. Alternative Names: Mubritinib; TAK165; TAK-165; TAK-165. CAS No. 366017-09-6. Pack Sizes: 50 mg. Product ID: B0084-067201. Molecular formula: C25H23F3N4O2. Mole weight: 468.48. Custom synthesis is available. Send your inquiries for more information. | London |
| Naquotinib | Naquotinib is an irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity with IC50 of 8-33 nM toward EGFR mutants. Group: Pharmaceutical. Alternative Names: ASP 8273; ASP8273; ASP-8273; (R)-5-((1-acryloylpyrrolidin-3-yl)oxy)-6-ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrazine-2-carboxamide. CAS No. 1448232-80-1. Pack Sizes: 5 mg. Product ID: B0084-475727. Molecular formula: C30H42N8O3. Mole weight: 562.719. Custom synthesis is available. Send your inquiries for more information. | London |
| Neratinib | Neratinib, also known as HKI-272 or PB272, is an orally available, 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Treatment of cells with this agent results in inhibition of downstream signal transduction events and cell cycle regulatory pathways; arrest at the G1-S (Gap 1/DNA synthesis)-phase transition of the cell division cycle; and ultimately decreased cellular proliferation. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells. Group: Pharmaceutical. Alternative Names: 2-Butenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-; (2E)-N-[4-[[3-Chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide; (E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide; (E)-N-[4-[[3-Chloro-4-((pyridin-2-yl)meth. CAS No. 698387-09-6. Pack Sizes: 500 mg. Product ID: B0084-347125. Molecular formula: C30H29ClN6O3. Mole weight: 557.04. Custom synthesis is available. Send your inquiries for more information. | London |
| Olmutinib | Olmutinib, also called as HM61713 and BI-1482694, is an orally available, mutant-selective third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that is being developed for treatment of advanced and metastatic EGFR mutation-positive non-small cell lung cancer (NSCLC). In May 2016, olmutinib received its first global approval in South Korea for the treatment of EGFR T790M mutation-positive lung cancer. Olmutinib is also a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). Group: Pharmaceutical. Alternative Names: N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide; HM61713; HM 61713; HM-61713; BI 1482694; BI-1482694; BI1482694; Olmutinib. CAS No. 1353550-13-6. Pack Sizes: 200 mg. Product ID: B0084-470842. Molecular formula: C26H26N6O2S. Mole weight: 486.18. Custom synthesis is available. Send your inquiries for more information. | London |
| Pyrotinib | Pyrotinib, also known as SHR-1258, is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. Upon oral administration, pyrotinib binds to and inhibits both EGFR and HER2, which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumor cells. Group: Pharmaceutical. Alternative Names: (R,E)-N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide; Pyrotinib; SHR-1258; SHR1258; SHR 1258; Pyrotinib maleate. CAS No. 1269662-73-8. Pack Sizes: 1 mg. Product ID: B0084-267738. Molecular formula: C32H31ClN6O3. Mole weight: 582.21. Custom synthesis is available. Send your inquiries for more information. | London |
| Rociletinib | Rociletinib is a third-generation irreversible kinase inhibitor of epidermal growth factor receptor (EGFR). Rociletinib was shown to inhibit the proliferation of non-small cell lung cancer (NSCLC) cells expressing mutant EGFR. It also exhibits anti-tumor activity in NSCLC EGFR mutant xenograft models. Group: Pharmaceutical. Alternative Names: CO-1686; CO1686; CO 1686; AVL-301; AVL 301; AVL301; CNX-419; CNX 419; CNX419; N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide. CAS No. 1374640-70-6. Pack Sizes: 100 mg. Product ID: B0084-462150. Molecular formula: C27H28F3N7O3. Mole weight: 555.562. Custom synthesis is available. Send your inquiries for more information. | London |
| SU 4312 | SU 4312 is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 = 0.8 and 19.4 μM, respectively) wirth selectivity over EGFR and c-Src tyrosine kinases. Group: Pharmaceutical. Alternative Names: SU4312; SU-4312; 3-[[4-(dimethylamino)phenyl]methylene]-1,3-dihydro-2H-indol-2-one; 2H-Indol-2-one, 3-[[4-(dimethylamino)phenyl]methylene]-1,3-dihydro-; 2-Indolinone, 3-[p-(dimethylamino)benzylidene]-; 3-(4-Dimethylaminobenzylidenyl)-2-indolinone; 3-[[4-(Dimethylamino)phenyl]methylidene]-2,3-dihydro-1H-indol-2-one; DMBI; NSC 86429. CAS No. 5812-7-7. Pack Sizes: 50 mg. Product ID: B0084-357203. Molecular formula: C17H16N2O. Mole weight: 264.33. Custom synthesis is available. Send your inquiries for more information. | London |
| Tyrphostin 9 | Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM. Group: Pharmaceutical. Alternative Names: Malonoben; SF 6847; SF6847; SF-6847; RG 50872; RG50872; RG-50872; 2,6-Di-tert-butyl-4-(2,2-dicyanovinyl)phenol. CAS No. 10537-47-0. Pack Sizes: 1 g. Product ID: B1370-358320. Molecular formula: C18H22N2O. Mole weight: 282.38. Custom synthesis is available. Send your inquiries for more information. | London |
| UNC2250 | UNC2250 is a potent and selective Mer Kinase inhibitor. When applied to live cells, UNC2250 inhibited steady-state phosphorylation of endogenous Mer with an IC50 of 9.8 nM and blocked ligand-stimulated activation of a chimeric EGFR-Mer protein. Treatment with UNC2250 also resulted in decreased colony-forming potential in rhabdoid and NSCLC tumor cells. The results provide a rationale for further investigation of UNC2250 for therapeutic application in patients with cancer. Group: Pharmaceutical. Alternative Names: UNC-2250; UNC 2250. CAS No. 1493694-70-4. Pack Sizes: 50 mg. Product ID: B2693-462617. Molecular formula: C24H36N6O2. Mole weight: 440.58. Custom synthesis is available. Send your inquiries for more information. | London |
| WZ-4002 | WZ-4002 is an EGFR phosphorylation inhibitor with selectivity for EGFR T790M. It has a framework of pyrimidine compound which is different from other EGFR inhibitors. WZ-4002 exhibits anti-tumor activity. Uses: Protein kinase inhibitors. Group: Pharmaceutical. Alternative Names: WZ4002; N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide; WZ 4002. CAS No. 1213269-23-8. Pack Sizes: 50 mg. Product ID: B0084-286777. Molecular formula: C25H27ClN6O3. Mole weight: 494.98. Custom synthesis is available. Send your inquiries for more information. | London |
| XL-647 | XL647 is an orally bioavailable small-molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity. It inhibits EGFR, HER2, VEGFR and EphB4 kinase. Group: Pharmaceutical. Alternative Names: XL-647; XL 647; XL647; EXEL-7647; EXEL 7647; EXEL7647; KD-019; KD 019; KD019. CAS No. 781613-23-8. Pack Sizes: 5 mg. Product ID: B0084-459630. Molecular formula: C24H25Cl2FN4O2. Mole weight: 491.39. Custom synthesis is available. Send your inquiries for more information. | London |
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