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.
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A novel potent, selective, and orally bioavailable RAF inhibitor with biochemical IC50 of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively; suppresses pERK (EC50=0.02-0.1 uM), stabilizes BRAF−CRAF dimers(EC50=0.8 uM) inhibits proliferation (EC50=0.95 uM) in KRAS mutant tumor cell lines (Calu6); shows effectivity in a KRAS mutant xenograft model.
BGB-283 (Lifirafenib, BGB283) is a potent pan RAF inhibitor of BRAF V600E, wt BRAF, CRAFY340/341D and wt ARAF (IC50=5-40 nM); inhibits recombinant BRAFV600E with IC50 of 23 nM; also inhibits EGFR and EGFR T790M/L858R with IC50 of 29 nM and 495 nM respectively; potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation in vitro; shows tumor growth inhibition in both cell line-derived and primary human colorectal tumor xenografts bearing BRAF(V600E) mutation.
CCT196969 is a potent, orally bioavailable pan-RAF inhibitor with IC50 of 100, 40 and 12 nM for B-Raf, B-Raf V600E and C-Raf, respectively; also potently inhibits SRC (IC50=26 nM) and LCK (IC50=14 nM), does not inhibit MEK1 or the MEK1 kinase COT; inhibits cell proliferation of BRAF-selective-inhibitor-resistant cells with mean GI50 of 0.4 uM, NRAS mutant melanoma cells (GI50=0.6 uM); induces caspase 3 and PARP cleavage, induces apoptosis, inhibits the growth of PLX4720-resistant A375 xenografts (A375/R) in mice, without causing any body weight loss.
BRAF inhibitor 13
A potent and selective B-Raf inhibitor with IC50 of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively; induces proliferation and hyperplasia in normal tissues of mice.
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.
A potent, oral, dual Raf/VEGFR-2 inhibitor with IC50 of 3-60 nM for C-Raf/B-Raf/B-Raf V600E, EC50 of 30 nM for VEGFR2 phosphorylation; blocks Raf-MEK-ERK signalling and significantly enhances TRAIL sensitivity in NCI-H727 and CM insulinoma cells; inhibits cell proliferation with IC50 of 0.83-5.54 uM in CRC cells, demonstrates significant anti-tumor activity in tumors of xenograft models.
B-Raf IN 1
A highlt potent and selective BRAF/CRAF inhibitor with IC50 of 24/25 nM, respectively; displays moderate selectivity over p38α (IC50=216 nM) and CAMKII (IC50=822 nM), high selectivity over CDK2, CDK4, PKCa, IKKb, JNK1, MK2, PKA, Src, MKK6, PLK1, p70S6K, PI3 Ka, and PDK1 (IC50>2 uM).
A potent Raf inhibitor.
LXH254 (LXH-254, LXH 254) is a novel potent, ATP-competitive pan-RAF inhibitor, binds to Raf proteins and inhibits Raf-mediated signal transduction pathways, inhibits proliferation of Raf-overexpressing tumor cells; demonstrates anti-proliferative activity in cell lines that contain a variety of mutations that activate MAPK signaling, blocks mutant RAS-driven signaling and cell proliferation; demonstrates tumor regression in several KRAS-mutant models including the NSCLC-derived Calu-6 (KRAS Q61K) and NCI-H358 (KRAS G12C), exhibits efficacy in numerous MAPK-driven human cancer cell lines and in xenograft tumors representing model tumors harboring human lesions in KRAS, NRAS and BRAF oncogenes.
L-779450 is a potent, ATP-competitive Raf kinase inhibitor with IC50 of 10 nM, displays >7, >30 and >70-fold selectivity over p38α, GSK3β and Lck respectively; suppresses DNA synthesis and induced apoptosis in hematopoietic FDC-P1 cells transformed to grow in response to either Raf-1 or A-Raf, L-779,450 is less effective on B-Raf- or MEK1-responsive cells, also suppresses DNA synthesis and induces apoptosis in Raf-responsive cells and the effects are more significant on Raf-responsive compared to cytokine-mediated growth.
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