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Raf

Inhibitors

Cat.No.  Name Information
M1988 Dabrafenib Dabrafenib (free base) (GSK2118436A) is a V600 mutant BRAF-specific inhibitor.
M3026 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
M1774 PLX-4720 PLX-4720 is a selective BRAFV600E inhibitor with the IC50 values of 160 nM and 130 nM for B-Raf and BRK respectively.
M1761 Vemurafenib Vemurafenib (PLX4032; RG7204; RO5185426) is the first and effective selective inhibitor of B-Raf, which can inhibit RAFV600E and C-RAF-1 activity with IC50 of 31 nM and 48 nM, respectively. Vemurafenib induces autophagy.
M2319 AZ628 AZ628 is a potent inhibitor for wild-type CRAF and BRAF V600E with IC50 of 29 nM and 34 nM, respectively.
M10880 Rineterkib hydrochloride Rineterkib hydrochloride (compound B) is an orally active inhibitor of RAF and ERK1/2 that exerts an antiproliferative effect by activating mutations in the MAPK pathway. This activity is particularly associated with KRAS-mutant non-small cell lung cancer, BRAF-mutant non-small cell lung cancer, KRAS-mutant pancreatic cancer, KRAS-mutant colon cancer, and KRAS mutant ovarian cancer.
M10733 Rineterkib Rineterkib (compound B) is an orally active inhibitor of RAF and ERK1/2 that exerts an antiproliferative effect by activating mutations in the MAPK pathway. This activity is particularly associated with KRAS-mutant non-small cell lung cancer, BRAF-mutant non-small cell lung cancer, KRAS-mutant pancreatic cancer, KRAS-mutant colon cancer, and KRAS-mutant ovarian cancer.
M10591 AZ304 AZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF with IC50 values of 79 nM and 38 nM respectively.
M10475 Lifirafenib (BGB-283) Lifirafenib (BGB-283) is a novel potent and selective RAF Kinase and EGFR inhibitor with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.
M10438 BI 882370 BI 882370 is a highly potent and selective RAF inhibitor that binds to the DFG-out (inactive) conformation of the BRAF kinase.
M10152 Naporafenib Naporafenib (also known as LXH254) is an orally available inhibitor of C-Raf and B-Raf with potential antineoplastic activity.
M9492 B-Raf inhibitor 1 B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 µM and 2 nM for A375 proliferation and A375 p-ERK, respectively.
M9008 PLX7904 PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor.
M9007 PLX8394 PLX8394 is an orally bioavailable, potent and selective Raf inhibitor with IC50 of 5 nM.
M8897 B-Raf-IN-1 B-Raf-IN-1 (MDK36057) is a potent b-Raf inhibitor with IC50 of 24 nM.
M8886 RAF709 RAF709 is a novel Raf kinase inhibitor with IC50 values of 0.4 and 1.5 nM for c-Raf and b-Raf, respectively.
M5327 L-779450 L-779450 is a potent, ATP-competitive Raf kinase inhibitor (IC50 =10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.
M3026 Sorafenib Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
M2927 PF-04880594 PF-04880594 is a RAF inhibitor for BRAF/BRAFV599E and c-RAF with IC50 of 0.19 nM/0.13 nM and 0.39 nM, >100-fold selectivity over CSNK1, JNK2/3 and p38.
M2813 LGX818 LGX818 is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM.
M2745 GW5074 GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted.
M2319 AZ628 AZ628 is a potent inhibitor for wild-type CRAF and BRAF V600E with IC50 of 29 nM and 34 nM, respectively.
M2235 TAK-632 TAK-632 is a potent and selective pan-RAF inhibitor.
M2090 MLN2480 MLN2480 (BIIB-024) is an oral, selective pan-Raf kinase inhibitor.
M2045 CEP-32496 CEP-32496 is a potent orally active BRAF inhibitor with IC50 of 14 nM.



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