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) | ||
|---|---|---|---|---|
| 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 |
| S8755 | AZ304 | <1 mg/mL | 90 mg/mL | 5 mg/mL |
| S7965 | PLX8394 | <1 mg/mL | 100 mg/mL | <1 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(RXDX-105) | <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（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-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。 |
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).
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| S1040 |
Sorafenib TosylateSorafenib 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。 |
Western blot analysis of proteins expression levels in pericytes at 5-hour treatment with DMSO (vehicle), 10 μmol/L vemurafenib (Vemu.), 2.5 μmol/L sorafenib (Sora.), and combined therapy with 10 μmol/L vemurafenib plus 2.5 μmol/L sorafenib. These results were validated by three independent replicate measurements. Cells were grown in 0.2% FBS DMEM growth medium during treatment.
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| S1152 |
PLX-4720PLX-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。 |
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.
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| 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。 |
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.
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| S1104 |
GDC-0879GDC-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。 |
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.
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| S8755New |
AZ304AZ304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。 |
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| S7965New |
PLX8394PLX8394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。 |
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| S8745New |
LXH254LXH254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。 |
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| S5069New |
Dabrafenib MesylateDabrafenib 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. |
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| S5077New |
Regorafenib MonohydrateRegorafenib 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。 |
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| S8690New |
RAF709RAF709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。 |
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| 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。 |
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).
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| S2746 |
AZ 628AZ 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。 |
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.
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| S2202 |
NVP-BHG712NVP-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。 |
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| S2220 |
SB590885SB590885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。 |
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.
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| S2720 |
ZM 336372ZM 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。 |
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.
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| S7397 |
SorafenibSorafenib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。 |
(A) and (C) qPCR showing the levels of HMGA2 and SOX9 mRNA in Hep3B and Huh7 human HCC cells treated for 48 hours with 1 μM AZD6244, or 7.5 μM sorafenib relative to control-treated cells (Ctrl). (B) and (D) qPCR showing Hmga2 and Sox9 expression in p53−/−; HRAS(G12V) and p53−/−; Myc; Cas9; sgNf1 mouse liver cells. Drug treatment was the same as in (A). Error bars are s.d. of mean (n = 3). ***, P < .001.
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| S2872 |
GW5074GW5074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。 |
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.
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| S7291 |
TAK-632TAK-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。 |
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.
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| S8015 |
CEP-32496(RXDX-105)CEP-32496是一种高度有效的BRAF(V600E/WT)和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。 |
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| 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。 |
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. |
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| 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。 |
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| S7743 |
CCT196969CCT196969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。 |
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| 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。 |
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| S7964 |
PLX7904PLX7904，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。 |
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| S7842 |
LY3009120LY03009120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。 |
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)
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| 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。 |
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| S7121 |
MLN2480MLN2480是一种口服的Raf激酶抑制剂。 |
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| S2200 |
Raf265 derivativeRaf265 derivative是Raf265的衍生物，其作用不明确。 |
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