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BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Group: Pharmaceutical. Alternative Names: BI-847325; BI 847325; BI847325. CAS No. 1207293-36-4. Pack Sizes: 10 mg. Product ID: B0084-470824. Molecular formula: C29H28N4O2. Mole weight: 464.56. Custom synthesis is available. Send your inquiries for more information.
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Binimetinib
Binimetinib is an oral, highly selective MEK inhibitor. Group: Pharmaceutical. Alternative Names: MEK162; MEK-162; MEK 162; ARRY162; ARRY-162; ARRY 162; ARRY438162, Binimetinib; 5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide. CAS No. 606143-89-9. Pack Sizes: 300 mg. Product ID: B0084-455720. Molecular formula: C17H15BrF2N4O3. Mole weight: 441.233. Custom synthesis is available. Send your inquiries for more information.
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Cobimetinib
Cobimetinib (GDC-0973, RG7420) is a potent, orally available and highly selective MEK1 inhibitor with IC50 of 4.2 nM. It shows more than 100-fold selectively for MEK1 over MEK2 when tested against a panel of more than 100 serine-threonine and tyrosine kinases and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Group: Pharmaceutical. Alternative Names: XL518; GDC-0973; RG7420. CAS No. 934660-93-2. Pack Sizes: 25 mg. Product ID: B0084-460683. Molecular formula: C21H21F3IN3O2. Mole weight: 531.31. Custom synthesis is available. Send your inquiries for more information.
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Encorafenib
Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Group: Pharmaceutical. Alternative Names: LGX818; LGX-818; LGX 818; Methyl N-[(2S)-1-[[4-[3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-propan-2-ylpyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate. CAS No. 1269440-17-6. Pack Sizes: 150 mg. Product ID: B0084-462563. Molecular formula: C22H27ClFN7O4S. Mole weight: 540.011. Custom synthesis is available. Send your inquiries for more information.
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PD0325901
PD-0325901 is a potent bioavailable and selective MEK inhibitor, which targets mitogen-activated protein kinase kinase (MAPK/ERK kinase or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI-1040, selectively binds to and inhibits MEK, which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors. Uses: Reprogramming, self-renewal. Group: Pharmaceutical. Alternative Names: PD 0325901; PD 325901. CAS No. 391210-10-9. Pack Sizes: 100 mg. Product ID: B0084-091588. Molecular formula: C16H14F3IN2O4. Mole weight: 482.198. Custom synthesis is available. Send your inquiries for more information.
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RGB-286638 Free base
RGB-286638 is a novel CDK inhibitor. It inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. It demonstrated equimolar (50nM) activity in freshly isolated tumor cells from MM patients, while manifesting less cytotoxicity in healthy donor PBMCs. It reduced the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but had no effects on p-Rb S780. Group: Pharmaceutical. Alternative Names: 1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[1,2-c]pyrazol-5-yl]-3-morpholin-4-ylurea; RGB 286638; RGB286638. CAS No. 784210-88-4. Pack Sizes: 100 mg. Product ID: B0084-463330. Molecular formula: C29H35N7O4. Mole weight: 545.63. Custom synthesis is available. Send your inquiries for more information.
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Thiazovivin
Thiazovivin is a selective, cell permeable small molecule that directly targets Rho-associated kinase (ROCK). In addition, Thiazovivin protects human embryonic stem cells (hESCs) in the absence of ECM by regulating E-cadherin mediated cell-cell interaction. This observation suggests that Thiazovivin promotes cell survival. In other studies Thiazovivin, in combination with inhibitors of the TGF-β receptor and MEK pathway, has shown to improve reprogramming efficiency by more than 200-fold. Uses: Reprogramming, self-renewal. Group: Pharmaceutical. Alternative Names: N-benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide; N-Benzyl-2-(pyrimidin-4-ylamino)-thiazole-4-carboxamide; N-(PHENYLMETHYL)-2-(4-PYRIMIDINYLAMINO)-4-THIAZOLECARBOXAMIDE; N-Benzyl-[2-(pyrimidin-4-yl)amino]thiazole-4-carboxamide; 4-THIAZOLECARBOXAMIDE, N-(PHENYLMETHYL)-2-(4-PYRIMIDINYLAMINO)-. CAS No. 1226056-71-8. Pack Sizes: 25 mg. Product ID: B0084-286727. Molecular formula: C15H13N5OS. Mole weight: 311.363. Custom synthesis is available. Send your inquiries for more information.
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Trametinib
A MEK inhibitor that suppresses MEK1 and MEK2 with IC50 of 0.92 and 1.8 nM and no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. It has been approved by FDA, in combination with Tafilnar, for the treatment of metastatic anaplastic thyroid cancer (ATC) with BRAF V600E mutation. Group: Pharmaceutical. Alternative Names: GSK-1120212; GSK 1120212; GSK1120212; JTP74057; JTP 74057; JTP-74057; Mekinist. CAS No. 871700-17-3. Pack Sizes: 500 mg. Product ID: B0084-307744. Molecular formula: C26H23FIN5O4. Mole weight: 615.39. Custom synthesis is available. Send your inquiries for more information.
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