B-Raf 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S1104 GDC-0879

GDC-0879是一种新型有效的,选择性B-Raf抑制剂,在A375和Colo205细胞中IC50为0.13 nM,对c-Raf也有抑制作用;对其他蛋白激酶没有抑制作用。

Selective B-Raf, IC50: 0.13 nM
S2220 SB590885

SB590885是一种有效的B-Raf抑制剂,无细胞试验中Ki为0.16 nM,作用于B-Raf比作用于c-Raf选择性高11倍,对其他人类激酶没有抑制作用。

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)是一种有效的选择性C-Raf/B-Raf/B-Raf V600E抑制剂,IC50为3-60 nM,对VEGFR2磷酸化表现出有效的抑制作用,无细胞试验中EC50为30 nM。Phase 2。

Selective B-Raf, IC50: 3 nM-60 nM
S7108 Encorafenib (LGX818)

Encorafenib (LGX818)是高效的RAF抑制剂,作用于表达B-RAF(V600E)的细胞,具有选择性的抗增殖和凋亡活性,EC50为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
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, IC50: 5.2 nM; B-Raf (V600E), IC50: 0.7 nM
S2807 Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436)是一种突变型BRAFV600特异性抑制剂,无细胞试验中IC50为0.7 nM,作用于B-Raf(wt)和c-Raf效果分别低7和9倍。

Pan B-Raf, IC50: 5.2 nM; B-Raf (V600E), IC50: 0.7 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 BRAF(V600E), IC50: 1 nM; B-Raf, IC50: 1.5 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
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, IC50: 14 nM; BRAF(V600E), IC50: 3.8 nM
S7842 LY3009120

LY03009120是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。Phase 1。

Pan BRAF(V600E), IC50: 5.8 nM; BRAF WT, IC50: 15 nM
S8853 Belvarafenib (HM95573)

Belvarafenib (GDC5573, HM95573, RG6185) 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 V600E, IC50: 7 nM; BRAF WT, IC50: 41 nM
S7170 RO5126766 (CH5126766)

RO5126766 (CH5126766)是一种双重RAF/MEK抑制剂,对BRAF V600E,BRAF,CRAF,和 MEK1的IC50分别为8.2 nM,19 nM,56 nM,和160 nM。Phase 1。

Pan BRAF, IC50: 19 nM; BRAF V600E, IC50: 8.2 nM
S7291 TAK-632

TAK-632是强效的泛Raf抑制剂,无细胞试验中对B-Raf(wt)和C-Raf的IC50分别为8.3 nM and 1.4 nM, 对其他被测试的酶抑制效果较差或者没有效果。

Pan B-Raf, IC50: 8.3 nM
S1152 PLX-4720

PLX-4720是一种有效的,选择性的B-RafV600E抑制剂,无细胞试验中IC50为13 nM,同样有效地作用于c-Raf-1(Y340D和Y341D突变型),作用于B-RafV600E比作用于野生型B-Raf选择性高10倍。

Pan B-Raf, IC50: 160 nM; B-Raf (V600E), IC50: 13 nM
S8015 Agerafenib (RXDX-105)

CEP-32496是一种高度有效的BRAF(V600E/WT)c-Raf抑制剂,Kd为14 nM/36 nM和39 nM,适度有效作用于Abl-1, c-Kit, Ret, PDGFRβ和VEGFR2,对MEK-1, MEK-2, ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。

Pan B-Raf, Kd: 36 nM; B-Raf (V600E), Kd: 14 nM
S5077 Regorafenib (BAY-734506) Monohydrate

Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) 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 (BAY 73-4506)

Regorafenib (BAY 73-4506)是一个多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR-β,Kit,RETRaf-1,在无细胞试验中IC50分别是13 nM,4.2 nM,46 nM,22 nM,7 nM,1.5 nM和2.5 nM。

Pan B-Raf, IC50: 28 nM; B-Raf (V600E), IC50: 19 nM
S7397 Sorafenib (BAY 43-9006)

Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂,无细胞试验中IC50分别为6 nM, 22 nM和90 nM。

Pan B-Raf (V599E), IC50: 38 nM; B-Raf, IC50: 22 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
S1040 Sorafenib (BAY 43-9006) tosylate

Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)RAF/MEK/ERK级联抑制剂,同时作用于Raf-1,wtBRAF和V599EBRAF,IC50分别为6 nM, 22 nM和38 nM。

Pan B-Raf (V599E), IC50: 38 nM; B-Raf, IC50: 22 nM
S7926 Lifirafenib (BGB-283)

Lifirafenib (BGB-283)有效地抑制RAF激酶家族和EGFR活性,在生化实验检测中,其对重组BRAF(V600E)激酶区域、EGFR和EGFR(T790M/L858R)突变体的IC50分别为23、29、495 nM。

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)是一种新型有效的B-RafV600E抑制剂,IC50为31 nM。Vemurafenib对B-RafV600E的选择性比对野生型B-Raf的选择性高10倍,在细胞实验中,选择性可高100倍以上。

Pan B-Raf, IC50: 100 nM; B-Raf (V600E), IC50: 31 nM
S2746 AZ 628

AZ 628是一种新型泛Raf抑制剂,作用于BRAF,BRAFV600E和c-Raf-1,无细胞试验中IC50分别为105 nM,34 nM和29 nM,也抑制VEGFR2, DDR2, Lyn, Flt1, FMS等。

Pan B-Raf, IC50: 105 nM; B-Raf (V600E), IC50: 34 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是一种新型的、具有口服活性的pan-RAF抑制剂,同时具有抑制SRC的活性。它还能抑制LCK和p38 MAPKs。

Pan BRAF, IC50: 0.1 μM