Raf

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抑制剂选择性比较

特异性亚型抑制剂

Raf产品

所有产品 Raf抑制剂(29) 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。	Cancer Discov, 2019, 9(7):852-871 Cancer Cell, 2019, 36(1):68-83 Mol Cell, 2019, 75(4):669-682	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。	Cancer Cell, 2019, 36(2):179-193 Cancer Lett, 2019, 454:14-25 J Exp Clin Cancer Res, 2019, 38(1):204	Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.
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。	Thyroid, 2019, 29(1):79-92 Oncogene, 2019, 38(22):4384-4396 Mol Cell Proteomics, 2019, 18(6):1096-1109	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。	Nat Commun, 2019, 10(1):2197 Cell Rep, 2019, 26(1):65-78 Cell Death Differ, 2019, 10.1038/s41418-019-0298-5	A375P cells were treated with vehicle, the BRAF inhibitor GSK2118436, the MEK inhibitor GSK1120212, 10 uM HCQ, or the indicated combinations. Shown are 48-hour immunoblots directed against the indicated proteins.
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。	ACS Med Chem Lett, 2018, 9(12):1199-1204 Med Oncol, 2017, 35(1):7 Nat Commun, 2016, 7:13781	Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.
S6538^New	B-Raf IN 1 B-Raf IN 1是Raf的抑制剂，对B-raf和C-raf的IC50值分别为24 nM和25 nM。它对Raf对具有高选择性，对13种其他激酶如PKCα, IKKβ和PI3Kα抑制活性较低。
S8755^New	AZ304 AZ304是一种合成的抑制剂，靶向野生型和V600E突变型的BRAF，IC50分别为79 nM和38 nM。它还能抑制CRAF, p38 和 CSF1R，IC50在100 nM以下。
S7965^New	PLX8394 PLX8394是一种具有口服活性的BRAF小分子抑制剂，对BRAF(V600E)、WT BRAF和CRAF的IC50分别为3.8 nM、14 nM和23 nM。它具有潜在的抗肿瘤活性。
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。	ACS Med Chem Lett, 2018, 9(12):1199-1204 Clin Cancer Res, 2017, 23(20):6203-6214 Br J Haematol, 2016, 175(4):641-651	Immunoblots showing levels of phospho-MEK (p-MEK), total MEK (t-MEK), phospho-ERK1/2 (p-ERK1/2) and total ERK1/2 (t-ERK1/2) in A375 cells transduced with a retrovirus expressing BRAFV600E, BRAFV600E/L505H, BRAFV600E/F516G or BRAFV600E/T529N and treated with increasing doses of RAF265. α-tubulin (TUBA) was monitored as a loading control.
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。	Mol Cell, 2019, 75(4):669-682 J Cell Mol Med, 2019, 10.1111/jcmm.14514 Stem Cell Reports, 2018, 11(2):380-394	Enzymatic activity of RIP3 from Abcam, the concentration-effect relationship of RIP3 inhibition by the tested protein kinase inhibitors and the mode of action of RIP3 inhibition by dabrafenib. The RIP3 inhibition rates of AZ628 at different concentrations were measured by the luminescent RIP3 assay. The data (mean ?SD from 3 independent experiments) were presented as the Lineweaver-Burk plots using Graphpad Prism 5.
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 Med Chem, 2019, 10.1021/acs.jmedchem.9b00855 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) Chembiochem, 2018, 10.1002/cbic.201800359 Elife, 2016, 10.7554/eLife.11999	Cell morphology of BCPAP, K1 and 8505C cells treated and untreated with SB590885 using IC50 dose. Massive vacuolization is easily visible around the nuclei in treated cells.
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。	Stem Cell Reports, 2018, 11(2):380-394 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。	Cell, 2019, 178(6):1478-1492 Cancer Discov, 2019, 9(1):46-63 Mol Cell, 2019, 75(4):669-682	Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.
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。	PLoS One, 2018, 13(9):e0203402 Gut, 2017, 66(6):1106-1115 Toxicology, 2017, 389:74-84	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。	ACS Med Chem Lett, 2018, 9(12):1199-1204 Anticancer Res, 2018, 38(11):6147-6156 Nutrients, 2017, 9(9)	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(RXDX-105) 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。	Mol Cell Biochem, 2019, 10.1007/s11010-019-03554-3 Cancer Discov, 2018, 8(9):1130-1141 Clin Proteomics, 2018, 15:13	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。
S8745	LXH254 LXH254是一种II型ATP竞争性抑制剂，抑制BRAF和CRAF的激酶活性，具有高选择性。
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。
S8690	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。
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。	Int J Cancer, 2018, 143(12):3131-3142 Chembiochem, 2018, 19(18):1988-1997
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。	Mol Cancer Ther, 2019, 18(7):1323-1334 Mol Cancer Res, 2019, 10.1158/1541-7786.MCR-18-1332 Cancer Discov, 2018, 8(9):1130-1141	B, VE or VELV were transiently transfected in SKBR3 for 24 hours. Then, the cells were treated with 1 μmol/L lapatinib for 1 hour, followed by treatment with DMSO or the RAF inhibitors indicated for 1 hour (the dose for vemurafenib, PLX7904, LY3009120, TAK632, BGB3245, and BGB3290 is 1 μmol/L; the dose for dabrafenib and PLX8394 is 300 nmol/L). Untransfected (UT) SKBR3 cells were treated with DMSO or 1 μmol/L lapatinib (lanes 1 and 2)
S5069	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.
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。	Int J Oncol, 2019, 54(2):515-526 Int J Mol Sci, 2018, 19(4) Nat Methods, 2018, 15(9):732-740
S5077	Regorafenib Monohydrate Regorafenib 瑞戈非尼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。
S7121	MLN2480 MLN2480是一种口服的Raf激酶抑制剂。

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。	Cancer Discov,2019, 9(7):852-871 Cancer Cell,2019, 36(1):68-83 Mol Cell,2019, 75(4):669-682	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。	Cancer Cell,2019, 36(2):179-193 Cancer Lett,2019, 454:14-25 J Exp Clin Cancer Res,2019, 38(1):204	Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.
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。	Thyroid,2019, 29(1):79-92 Oncogene,2019, 38(22):4384-4396 Mol Cell Proteomics,2019, 18(6):1096-1109	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。	Nat Commun,2019, 10(1):2197 Cell Rep,2019, 26(1):65-78 Cell Death Differ,2019, 10.1038/s41418-019-0298-5	A375P cells were treated with vehicle, the BRAF inhibitor GSK2118436, the MEK inhibitor GSK1120212, 10 uM HCQ, or the indicated combinations. Shown are 48-hour immunoblots directed against the indicated proteins.
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。	ACS Med Chem Lett,2018, 9(12):1199-1204 Med Oncol,2017, 35(1):7 Nat Commun,2016, 7:13781	Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.
S6538^New	B-Raf IN 1 B-Raf IN 1是Raf的抑制剂，对B-raf和C-raf的IC50值分别为24 nM和25 nM。它对Raf对具有高选择性，对13种其他激酶如PKCα, IKKβ和PI3Kα抑制活性较低。
S8755^New	AZ304 AZ304是一种合成的抑制剂，靶向野生型和V600E突变型的BRAF，IC50分别为79 nM和38 nM。它还能抑制CRAF, p38 和 CSF1R，IC50在100 nM以下。
S7965^New	PLX8394 PLX8394是一种具有口服活性的BRAF小分子抑制剂，对BRAF(V600E)、WT BRAF和CRAF的IC50分别为3.8 nM、14 nM和23 nM。它具有潜在的抗肿瘤活性。
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。	ACS Med Chem Lett,2018, 9(12):1199-1204 Clin Cancer Res,2017, 23(20):6203-6214 Br J Haematol,2016, 175(4):641-651	Immunoblots showing levels of phospho-MEK (p-MEK), total MEK (t-MEK), phospho-ERK1/2 (p-ERK1/2) and total ERK1/2 (t-ERK1/2) in A375 cells transduced with a retrovirus expressing BRAFV600E, BRAFV600E/L505H, BRAFV600E/F516G or BRAFV600E/T529N and treated with increasing doses of RAF265. α-tubulin (TUBA) was monitored as a loading control.
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。	Mol Cell,2019, 75(4):669-682 J Cell Mol Med,2019, 10.1111/jcmm.14514 Stem Cell Reports,2018, 11(2):380-394	Enzymatic activity of RIP3 from Abcam, the concentration-effect relationship of RIP3 inhibition by the tested protein kinase inhibitors and the mode of action of RIP3 inhibition by dabrafenib. The RIP3 inhibition rates of AZ628 at different concentrations were measured by the luminescent RIP3 assay. The data (mean ?SD from 3 independent experiments) were presented as the Lineweaver-Burk plots using Graphpad Prism 5.
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 Med Chem,2019, 10.1021/acs.jmedchem.9b00855 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) Chembiochem,2018, 10.1002/cbic.201800359 Elife,2016, 10.7554/eLife.11999	Cell morphology of BCPAP, K1 and 8505C cells treated and untreated with SB590885 using IC50 dose. Massive vacuolization is easily visible around the nuclei in treated cells.
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。	Stem Cell Reports,2018, 11(2):380-394 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。	Cell,2019, 178(6):1478-1492 Cancer Discov,2019, 9(1):46-63 Mol Cell,2019, 75(4):669-682	Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.
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。	PLoS One,2018, 13(9):e0203402 Gut,2017, 66(6):1106-1115 Toxicology,2017, 389:74-84	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。	ACS Med Chem Lett,2018, 9(12):1199-1204 Anticancer Res,2018, 38(11):6147-6156 Nutrients,2017, 9(9)	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(RXDX-105) 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。	Mol Cell Biochem,2019, 10.1007/s11010-019-03554-3 Cancer Discov,2018, 8(9):1130-1141 Clin Proteomics,2018, 15:13	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。
S8745	LXH254 LXH254是一种II型ATP竞争性抑制剂，抑制BRAF和CRAF的激酶活性，具有高选择性。
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。
S8690	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。
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。	Int J Cancer,2018, 143(12):3131-3142 Chembiochem,2018, 19(18):1988-1997
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。	Mol Cancer Ther,2019, 18(7):1323-1334 Mol Cancer Res,2019, 10.1158/1541-7786.MCR-18-1332 Cancer Discov,2018, 8(9):1130-1141	B, VE or VELV were transiently transfected in SKBR3 for 24 hours. Then, the cells were treated with 1 μmol/L lapatinib for 1 hour, followed by treatment with DMSO or the RAF inhibitors indicated for 1 hour (the dose for vemurafenib, PLX7904, LY3009120, TAK632, BGB3245, and BGB3290 is 1 μmol/L; the dose for dabrafenib and PLX8394 is 300 nmol/L). Untransfected (UT) SKBR3 cells were treated with DMSO or 1 μmol/L lapatinib (lanes 1 and 2)
S5069	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.
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。	Int J Oncol,2019, 54(2):515-526 Int J Mol Sci,2018, 19(4) Nat Methods,2018, 15(9):732-740
S5077	Regorafenib Monohydrate Regorafenib 瑞戈非尼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。
S7121	MLN2480 MLN2480是一种口服的Raf激酶抑制剂。

研究领域

产品类型

Raf

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

Raf产品