C-Raf/Raf-1
B-Raf
A-raf

B-Raf 選擇性抑制劑

目錄號(hào)	產(chǎn)品名	產(chǎn)品描述	Selective / Pan	IC50 / Ki
S1104	GDC-0879	GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.	Selective	B-Raf, IC50: 0.13 nM
S2220	SB590885	SB590885 is a potent B-Raf inhibitor with K_i of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.	Selective	B-Raf, Ki: 0.16 nM
S6680	L-779450	L-779450 is a highly potent low nanomolar inhibitor of B-raf with IC50 of 10 nM and Kd of 2.4 nM.	Selective	B-Raf, IC50: 10 nM; B-Raf, Kd: 2.4 nM
S2161	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.	Selective	B-Raf, IC50: 3 nM-60 nM
S7108	Encorafenib	Encorafenib is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3.	Selective
S8745	Naporafenib (LXH254)	Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.	Pan
S2807	Dabrafenib	Dabrafenib is a mutant BRAF^V600E specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.	Pan	B-Raf (V600E), IC50: 0.7 nM; B-Raf, IC50: 5.2 nM
S5069	Dabrafenib Mesylate	Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.	Pan	B-Raf (V600E), IC50: 0.7 nM; B-Raf, IC50: 5.2 nM
S6660	B-Raf inhibitor 1 (Compound 13) dihydrochloride	B-Raf inhibitor 1 (Compound 13) is a type IIA Raf inhibitor which bind to the DFG-out conformation with ki of 1 nM,1 nM,and 0.3 nM for B-Raf(WT), B-Raf(V600E) and C-Raf, respectively.	Pan	B-Raf(V600E), Ki: 1 nM
S8690	RAF709	RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM.	Pan	B-Raf, IC50: 1.5 nM; BRAF(V600E), IC50: 1 nM
S7965	PLX8394	PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.	Pan	BRAF(V600E), IC50: 3.8 nM; BRAF, IC50: 14 nM
S7842	LY3009120	LY03009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. LY03009120 induces autophagy. Phase 1.	Pan	BRAF(V600E), IC50: 5.8 nM; BRAF WT, IC50: 15 nM
S8853	Belvarafenib	Belvarafenib is a selective and orally bioavailable pan-RAF kinase inhibitor with IC50 values of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF(V600E) and CRAF kinases, respectively.	Pan	BRAF WT, IC50: 41 nM; BRAF V600E, IC50: 7 nM
S7170	Avutometinib	Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.	Pan	BRAF V600E, IC50: 8.2 nM; BRAF, IC50: 19 nM
S7291	TAK-632	TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases.	Pan	B-Raf, IC50: 8.3 nM
S1152	PLX-4720	PLX4720 is a potent and selective inhibitor of B-Raf^V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.	Pan	B-Raf (V600E), IC50: 13 nM; B-Raf, IC50: 160 nM
S8015	Agerafenib (RXDX-105)	Agerafenib (RXDX-105, CEP-32496) is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with K_d of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret (c-Ret), PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.	Pan	B-Raf (V600E), Kd: 14 nM; B-Raf, Kd: 36 nM
S5077	Regorafenib (BAY-734506) Monohydrate	Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.	Pan	B-Raf, IC50: 28 nM; B-Raf (V600E), IC50: 19 nM
S1178	Regorafenib	Regorafenib is a multi-target inhibitor for?VEGFR1,?VEGFR2,?VEGFR3,?PDGFRβ,?Kit (c-Kit),?RET (c-RET)?and?Raf-1?with?IC50?of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces?autophagy.	Pan	B-Raf (V600E), IC50: 19 nM; B-Raf, IC50: 28 nM
S9621	Donafenib (Sorafenib D3)	Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively.	Pan	B-Raf, IC50: 22 nM
S7397	Sorafenib	Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.	Pan	B-Raf, IC50: 22 nM; B-Raf (V599E), IC50: 38 nM
S1040	Sorafenib tosylate	Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.	Pan	B-Raf, IC50: 22 nM; B-Raf (V599E), IC50: 38 nM
S7926	Lifirafenib (BGB-283)	Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.	Pan	BRAF(V600E), IC50: 23 nM; BRAF WT, IC50: 32 nM
S6538	B-Raf IN 1	B-Raf IN 1 is an inhibitor of Raf wih IC50 values of 24 nM and 25 nM for B-Raf and C-Raf respectively. It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα.	Pan	B-Raf, IC50: 24 nM
S1267	Vemurafenib (PLX4032)	Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.	Pan	B-Raf (V600E), IC50: 31 nM; B-Raf, IC50: 100 nM
S2746	AZ 628	AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 induces apoptosis.	Pan	B-Raf (V600E), IC50: 34 nM; B-Raf, IC50: 105 nM
S8755	AZ304	AZ304 is a synthetic inhibitor designed to interact with the ATP-binding site of wild type and V600E mutant BRAF with IC50 values of 79?nM and 38?nM, respectively. It also inhibits CRAF, p38 and CSF1R at sub 100?nM potencies.	Pan	WT BRAF, IC50: 79 nM; BRAF(V600E), IC50: 38 nM
S7743	CCT196969	CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.	Pan	BRAF, IC50: 0.1 μM