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

C-Raf/Raf-1 選擇性抑制劑

目錄號(hào)	產(chǎn)品名	產(chǎn)品描述	Selective / Pan	IC50 / Ki
S4947	Regorafenib Hydrochloride	Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, 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, respectively.	Selective	Raf-1, IC50: 2.5 nM
S2872	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. GW5074 inhibits LK-induced apoptosis.	Selective	C-Raf, IC50: 9 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.	Selective	CRAF, IC50: 0.01 μM
S8189	BAW2881 (NVP-BAW2881)	BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.	Selective	C-Raf-1, IC50: 24 nM
S2720	ZM 336372	ZM 336372 (Zinc00581684) is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.	Selective	C-Raf, IC50: 70 nM
S2202	NVP-BHG712	NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.	Selective	C-Raf, IC50: 0.395 μM
S1574	Doramapimod (BIRB 796)	Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.	Selective
S6905	MCP110	MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors.	Selective
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	C-Raf, Ki: 0.3 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	C-Raf, IC50: 0.4 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	C-Raf, IC50: 1.4 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	CRAF, IC50: 2 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	Raf-1, IC50: 2.5 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	Raf-1, IC50: 2.5 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	C-Raf, IC50: 4.3 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	Raf-1, IC50: 6 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	Raf-1, IC50: 6 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	Raf-1, IC50: 6 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	C-Raf, IC50: 6.3 nM
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	C-Raf, IC50: 6.3 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	C-Raf-1 (Y340D/Y341D), IC50: 6.7 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	C-RAF (Y340/341D), IC50: 7 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	CRAF, IC50: 23 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	C-Raf, IC50: 25 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	C-Raf-1, IC50: 29 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	C-Raf, Kd: 39 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	C-Raf, IC50: 48 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	CRAF, IC50: 56 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	CRAF, IC50: 68 nM
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