Raf

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1267	Vemurafenib (PLX4032, RG7204)	<1 mg/mL	97 mg/mL	<1 mg/mL
S1040	Sorafenib Tosylate	0.01 mg/mL	127 mg/mL	<1 mg/mL
S1152	PLX-4720	<1 mg/mL	83 mg/mL	<1 mg/mL
S2807	Dabrafenib (GSK2118436)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1104	GDC-0879	<1 mg/mL	66 mg/mL	5 mg/mL
S8745	LXH254	<1 mg/mL	100 mg/mL	34 mg/mL
S5069	Dabrafenib Mesylate	<1 mg/mL	100 mg/mL	5 mg/mL
S5077	Regorafenib Monohydrate	-1 mg/mL	100 mg/mL	-1 mg/mL
S8690	RAF709	<1 mg/mL	100 mg/mL	100 mg/mL
S2161	RAF265 (CHIR-265)	<1 mg/mL	100 mg/mL	33 mg/mL
S2746	AZ 628	<1 mg/mL	90 mg/mL	<1 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2220	SB590885	<1 mg/mL	5 mg/mL	<1 mg/mL
S2720	ZM 336372	<1 mg/mL	78 mg/mL	2 mg/mL
S7397	Sorafenib	<1 mg/mL	63 mg/mL	<1 mg/mL
S2872	GW5074	<1 mg/mL	104 mg/mL	<1 mg/mL
S7291	TAK-632	<1 mg/mL	100 mg/mL	2 mg/mL
S8015	CEP-32496	<1 mg/mL	9 mg/mL	<1 mg/mL
S7108	Encorafenib (LGX818)	<1 mg/mL	100 mg/mL	100 mg/mL
S8189	BAW2881 (NVP-BAW2881)	<1 mg/mL	84 mg/mL	20 mg/mL
S7743	CCT196969	<1 mg/mL	100 mg/mL	<1 mg/mL
S7926	Lifirafenib (BGB-283)	<1 mg/mL	95 mg/mL	95 mg/mL
S7964	PLX7904	<1 mg/mL	100 mg/mL	<1 mg/mL
S7842	LY3009120	<1 mg/mL	3 mg/mL	<1 mg/mL
S7170	RO5126766 (CH5126766)	<1 mg/mL	94 mg/mL	<1 mg/mL
S7121	MLN2480	<1 mg/mL	100 mg/mL	100 mg/mL
S2200	Raf265 derivative	<1 mg/mL	101 mg/mL	101 mg/mL

特异性亚型抑制剂

Raf抑制剂（27）
新Raf产品

产品目录	产品描述	文献引用	实验数据
S1267	Vemurafenib (PLX4032, RG7204) Vemurafenib (PLX4032, RG7204)是一种新型有效的B-Raf^V600E抑制剂，IC50为31 nM。Vemurafenib对B-Raf^V600E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。	Nature, 2017, 547(7664):453-457 Nature, 2016, 538(7626):477-482 Nature, 2017, 546(7658):431-435	The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).
S1040	Sorafenib Tosylate Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)和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。	Blood, 2012, 120(19):4104-15 Blood, 2013, 122(9):1621-33 Hepatology, 2013, 59(4):1435-47	Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 μM), JNK inhibitor (16 μM), p38 inhibitor SB203580 (20 μM), and multikinase inhibitor sorafenib (10 μM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.
S1152	PLX-4720 PLX-4720是一种有效的，选择性的B-Raf^V600E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。	Nature, 2013, 498(7452):109-12 Nature, 2015, 517(7536):583-8 Nature, 2012, 483(7387):100-3	Combinatorial knockdown of NF1 and C-RAF abrogates NF1-mediated resistance to B-RAF inhibition at the level of ERK phosphorylation. A375 cells were infected with NF1 shRNA and treated with either DMSO or PLX4720 for 16 h. Cell lysates were analyzed for the indicated proteins.
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。	Science, 2016, 352(6282):189-96 Cell, 2018, 173(6):1413-1425 Cell Res, 2015, 10.1038/cr.2015.56	BRAFi/MEKi-resistant A375DR and the parental A375 cells were treated with 2 μM vorinostat and/or the combination of 0.125 μM dabrafenib and 5 nM trametinib. Protein lysates were harvested after 72 hr. Western blot analysis was carried out for p-MEK and p-P90RSK as indicators of activation of MAPK pathway, ac-H3 as indicator for levels of acetylated histone H3 and a-tubulin as a loading control.
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。	Cancer Discov, 2013, 3(3):350-62 Nat Commun, 2016, 7:13781 J Natl Cancer Inst, 2012, 104(21):1673-9	Effect of RAF or multikinase inhibitors on RAF1-proficient and -deficient DIH. Immunoblot analysis of DIH treated with GDC-0879 (GDC), Sorafenib (SOR) or PP2. Proliferation was assessed after a 48 h treatment, and immunoblotting after 1 h treatment. TUBA, loading control.
S8745^New	LXH254 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.
S5069^New	Dabrafenib Mesylate Dabrafenib Mesylate is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.7 nM, 5.2 nM and 6.3 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.
S5077^New	Regorafenib Monohydrate Regorafenib是一种新型口服的多重激酶抑制剂，对VEGFR1、小鼠VEGFR2、小鼠VEGFR3、PDGFR-β、KIT、RET、RAF-1、B-RAF和B-RAF(V600E)的IC50分别为13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM。
S8690^New	RAF709 RAF709是有效的B/C RAF抑制剂，对C-RAF和B-RAF的IC50值分别为0.4 nM和1.5 nM。它具有高选择性，在浓度为1 μM时，对BRAF, BRAFV600E 和 CRAF的靶向结合率大于99%，而对DDR1、DDR2、FRK和FDGFRβ的脱靶效应非常少。
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。	Hepatology, 2012, 56(6):2363-74 Pigment Cell Melanoma Res, 2014, 27(1):124-33 Mol Cell Proteomics, 2012, 11(6):M112.017764	Raf265 inhibited the kinase activity of B-Raf but not of Raf-1 in Pkd2cKO cholangiocytes. Cells were treated for 30 min with different concentrations of Raf265. B-Raf and Raf-1 were immunoprecipated as described in the methods section and a kinase assay in vitro was performed using MEK as a substrate. The kinase activity of Raf was assessed by immunoblot analysis and quantified as optical density of pMEK with respect to untreated cells. In WT cholangiocytes (A) Raf265 inhibited both B-Raf and Raf-1 kinase activity. In Pkd2cKO cholangiocytes (B), Raf265 inhibited only B-Raf while a biphasic effect was found in Raf-1 with a significant increase at doses from 0.001 to 1 uM and a significant inhibition at 10 uM. Blots are representative of four different experiments. (p<0.05 vs controls; *p<0.001 vs controls).
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。	Cancer Discov, 2013, 3(3):350-62 J Med Chem, 2015, Cell Death Dis, 2014, 5:e1278	A375 cells were infected with the indicated shRNAs/ORFs. In parallel to the above, cells were also treated with 0.2 uM AZ628 for 16 h, cell lysates were analyzed by Western blotting for the indicated proteins.
S2202	NVP-BHG712 NVP-BHG712是一种特异性的EphB4抑制剂，ED50为25 nM，区别于对VEGFR和EphB4的抑制，对c-Raf， c-Src和c-Abl也具有抑制活性，IC50分别为0.395 μM， 1.266 μM和1.667 μM。	J Pharmacol Sci, 2015, 129(1):65-71 Anticancer Res, 2014, 34(6):2913-8
S2220	SB590885 SB590885是一种有效的B-Raf抑制剂，无细胞试验中K_i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。	Science, 2018, 361(6405) Elife, 2016, 10.7554/eLife.11999 Cell Death Dis, 2014, 5:e1278	Western blotting of the indicated proteins in WM266-4 cells treated for 48 h with 1 μM of BRAF (PLX4032 or SB590885) or MEK (AZD6244 or AS703026) inhibitors.
S2720	ZM 336372 ZM 336372是一种有效的，选择性的c-Raf抑制剂，IC50为70 nM，比作用于B-RAF选择性高10倍，对PKA/B/C， AMPK， p70S6等没有抑制作用。	Pharm Biol, 2016, 54(4):732-9	Effect of inhibitors on EAP’s proliferation activity in NIH3T3 cell by MTT assay. Data are presented as mean ± SD of three independent experiments. **p50.01 versus EAP.
S7397	Sorafenib 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。	Cancer Discov, 2015, 10.1158/2159-8290.CD-15-0913 Blood, 2012, 120(19):4104-15 Blood, 2013, 122(9):1621-33	Sorafenib in combination with metformin or the AMPK activator salicylate enhances AMPK activation. a, b, AMPK activation with the combination of sorafenib and metformin in LKB1 mutant KRAS mutant (A549 and H460) NSCLC cells (a), LKB1 wild-type KRAS mutant (H358) (b, left panel) or LKB1 mutant KRAS wild-type (H838) NSCLC cells (b, right panel). Cells were treated for 48 hr with sorafenib (1-3 uM), metformin (1–1.5 mM) or the combination of sorafenib and metformin with the same concentrations as were used for the individual treatments. c, AMPK activation with the combination of sorafenib and salicylate in LKB1 mutant KRAS mutant (A549 and H460) or LKB1 mutant KRAS wild-type (H838) NSCLC cells. Cells were treated for 48 hr with sorafenib (1–3 uM), salicylate (1–1.5 mM) or the combination of sorafenib and salicylate with the same concentrations as were used for the individual treatments. Cell lysates were harvested for western blot analysis and probed with the indicated antibodies.
S2872	GW5074 GW5074是一种有效的，选择性的c-Raf抑制剂，IC50为9 nM，对JNK1/2/3， MEK1， MKK6/7， CDK1/2， c-Src， p38 MAP， VEGFR2和c-Fms没有抑制活性。	Clin Cancer Res, 2015, 21(19):4420-30 Clin Cancer Res, 2014, 20(9):2410-23 Mol Cell Proteomics, 2012, 11(9):745-57	Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 °C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle-alone control, 27 °C represents temperature rescue of F508-CFTR at 27 °C, 37 °C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity.
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。	Oncotarget, 2016, 7(7):8172-83	Graph showing a concentration-dependent response of hypoxia-induced HIF-1α-NanoLuc activity to RAS-RAF-MEK-ERK pathway inhibitors: GDC-0994, PD-184352, selumetinib, TAK632, trametinib, and vemurafenib.
S8015	CEP-32496 CEP-32496是一种高度有效的BRAF(V600E/WT)和c-Raf抑制剂，K_d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。
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。	Clin Cancer Res, 2017, 10.1158/1078-0432.CCR-17-0098 Cancer Lett, 2016, 370(2):332-44	Whole cell lysates from NRAS- or BRAF-mutant melanoma cells treated with encorafenib or/and binimetinib or DMSO as a control for 24 h were subjected to Western blot analysis to detect pERK, ERK and β-Actin. Experiment shown is a representative of three independent experiments.
S8189	BAW2881 (NVP-BAW2881) BAW2881 (NVP-BAW2881)是一种新型的VEGFR酪氨酸激酶抑制剂。在1.0-4.3 nM浓度下能有效地抑制VEGFR1-3；在45-72 nM的浓度下，抑制PDGFRβ, c-Kit和RET。
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。
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。
S7964	PLX7904 PLX7904，又名PB04，是一种有效的、选择性RAF抑制剂。它能够在BRAF突变的黑色素瘤细胞中有效地抑制ERK1/2的激活，但在表达突变RAS的细胞中并不过度激活ERK1/2。
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。	Leukemia, 2017, 31(4):922-933 Cell Rep, 2016, 10.1016/j.celrep.2016.05.064	(a) INA-6, MM.1S, KMS11 or U266 cells were treated for 24 h either with 50 μm of the pan-Raf inhibitor MLN-2480, or 20 μm (INA-6 and MM.1S) or 25 μm (KMS11 or U266) of the pan-Raf inhibitor LY3009120 before western analyses of MEK1/2 and ERK1/2 activation with phosphorylation-specific antibodies.
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。
S7121	MLN2480 MLN2480是一种口服的Raf激酶抑制剂。
S2200	Raf265 derivative Raf265 derivative是Raf265的衍生物，其作用不明确。

研究领域

产品类型

Raf

信号通路图

研究领域

特异性亚型抑制剂