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Raf kinases are a family of three serine/threonine-specific protein kinases that are related to retroviral oncogenes. RAF is an acronym for Rapidly Accelerated Fibrosarcoma. Raf kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade. Activation of RAF kinases requires interaction with RAS-GTPases. The three RAF kinase family members are: A-Raf, B-Raf, C-Raf (Raf-1). The B-Raf protein is involved in sending signals inside cells, which are involved in directing cell growth. It was shown to be faulty (mutated) in some human cancers. C-RAF or even Raf-1 is an enzyme that in humans is encoded by the RAF1 gene. The c-Raf protein is part of the ERK1/2 pathway as a MAP kinase kinase kinase (MAP3K) that functions downstream of the Ras subfamily of membrane associated GTPases. C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases, from the TKL (Tyrosine-kinase-like) group of kinases.

Cat. No.	Product Name	CAS No.	Information
H7490	ZM 336372	208260-29-1	ZM 336372 is a potent, specific inhibitor of Raf isoforms in vitro (c-Raf IC50=70 nM), paradoxically induces >100-fold activation of c-Raf (Raf-1 activator), but without triggering any activation of MKK1 or p42 MAPK/ERK2; suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells, with marked induction of the cell cycle inhibitors p21 and p18; blocks cellular proliferation and suppresses NE vasoactive peptide production in pheochromocytoma cells.
H7489	XL-281	870603-16-0	XL-281 (BMS 908662) is a potent, selective, orally active inhibitor of wild-type and mutant RAF kinases with anti-tumor activity in multiple xenograft models; demonstrates biological activity by modulation of the RAF pathway in tumor and surrogate tissue, with decreases in cell proliferation and increases in apoptosis.
H7488	Vemurafenib	918504-65-1	Vemurafenib (PLX-4032;RG7204;RO5185426) is a potent, selective B-RAF V600E inhibitor with IC50 of 30 nM, displays similar potency for c-RAF-1 (IC50=48 nM), and has selectivity against many other kinases, including wild type B-RAF (IC50=100nM); potently inhibits proliferation of a panel of tumor cell lines, selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells; causes tumor regressions and improves animal survival in tumor xenograft models of BRAF(V600E)-expressing melanoma.
H7487	Sorafenib tosylate	475207-59-1	A potent, orally available Raf inhibitor with IC50 of 6, 22, and 38 nM for Raf-1, wt Braf, and BRaf V599E, respectively; Also demonstrates potent inhibition of certain proangiogenic RTKs, including VEGFR-2, PDGFR-β, VEGFR-3, Flt-3, c-Kit (IC50<100 nM); Exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
H7486	Sorafenib	284461-73-0	A potent, orally available Raf inhibitor with IC50 of 6, 22, and 38 nM for Raf-1, wt Braf, and BRaf V599E, respectively; Also demonstrates potent inhibition of certain proangiogenic RTKs, including VEGFR-2, PDGFR-β, VEGFR-3, Flt-3, c-Kit (IC50<100 nM); Exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
H7485	SB-699393	1348166-93-7	SB-699393 is a potent, selective and CNS penetrant B-Raf inhibitor with Kd of 7.2 nM; possesses enhanced CNS penetration (BB ratio=0.8:1) compared with SB-590885.
H7484	SB-590885	405554-55-4	A potent and selective B-Raf inhibitor with Kd of 0.3 nM; >1000 fold selectivity over p38a, GSK3b and Lck;
H7483	RRD-251 hydrochloride	72214-67-6	RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding; inhibits Rb to recruit Raf-1 to proliferative promoters and inhibited E2F1-dependent transcriptional activity; inhibits anchorage-dependent and anchorage-independent growth of human cancer cells; significantly inhibits tumor growth in tumors with functional Rb in vivo.
H7482	RRD-251	131916-62-6	RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding; inhibits Rb to recruit Raf-1 to proliferative promoters and inhibited E2F1-dependent transcriptional activity; inhibits anchorage-dependent and anchorage-independent growth of human cancer cells; significantly inhibits tumor growth in tumors with functional Rb in vivo.
H7481	REDX-05358	1884226-20-3	REDX-05358 is a novel potent, highly selective, orally bioavailable pan RAF inhibitor with IC50 of 0.1, 0.68, 0.171, and 0.076 nM for ARAF, BRAF, BRAF (V600E), and CRAF, respectively; denmonstrates high selectivity profile against a panel of 468 kinases, exhibits negligible paradoxical activation due to inhibition of both RAF monomers and dimers; not only inhibits MAPK signalling in BRAF V600E mutant tumor cells, but also in those harbouring NRAS and KRAS mutations; exhibits in vivo efficacy in BRAF V600E CRC xenograft model.

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