RO5126766(CH5126766)
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- CAS号:
- 946128-88-7
- 英文名:
- RO5126766(CH5126766)
- 英文别名:
- CH5126766;CS-1469;Avutometinib;RO5126766(CH5126766);3-{2-(methylaminosulfonyl)amino-3-fluoropyridin-4-ylmethyl}-4-methyl-7-(pyrimidin-2-yloxy)-2-oxo-2H-1-benzopyran;Sulfamide, N-[3-fluoro-4-[[4-methyl-2-oxo-7-(2-pyrimidinyloxy)-2H-1-benzopyran-3-yl]methyl]-2-pyridinyl]-N'-methyl-;3-[[2-[(Methylaminosulfonyl)amino]-3-fluoropyridin-4-yl]methyl]-4-methyl-7-[(pyrimidin-2-yl)oxy]-2H-1-benzopyran-2-one;MAPKK,CH 5126766,MEK,Ro 5126766,Raf kinases,Raf,Mitogen-activated protein kinase kinase,inhibit,Ro-5126766,CH-5126766,MAP2K,Inhibitor;3-[(2-((N-methylsulfamoyl)amino)-3-fluoropyridin-4-yl)methyl]-4-methyl-7-(pyrimidin-2-yloxy)-chromen-2-one,3-{2-(methylaminosulfonyl)amino-3-;RO5126766(CH5126766) 3-[[2-[(Methylaminosulfonyl)amino]-3-fluoropyridin-4-yl]methyl]-4-methyl-7-[(pyrimidin-2-yl)oxy]-2H-1-benzopyran-2-one
- 中文名:
- RO5126766(CH5126766)
- 中文别名:
- 化合物RO5126766;N-[3-氟-4-[[4-甲基-2-氧代-7-(2-嘧啶氧基)-2H-1-苯并吡喃-3-基]甲基]-2-吡啶]-N′-甲磺酰胺;3-[2-[(甲氨基磺酰基)氨基]-3-氟吡啶-4-基]甲基]-4-甲基-7-[(嘧啶-2-基)氧]-2H-1-苯并吡喃-2-酮
- CBNumber:
- CB82712006
- 分子式:
- C21H18FN5O5S
- 分子量:
- 471.46
- MOL File:
- 946128-88-7.mol
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RO5126766(CH5126766)化学性质
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沸点:
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690.8±65.0 °C(Predicted)
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密度:
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1.495±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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insoluble in H2O; insoluble in EtOH; ≥35.7 mg/mL in DMSO
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形态:
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Powder
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酸度系数(pKa):
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6.60±0.50(Predicted)
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RO5126766(CH5126766)性质、用途与生产工艺
RO5126766 (CH5126766, VS 6766, CKI-27, R-7304, RG-7304)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。
Target | Value |
BRAF V600E
(cell-free assay)
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8.2 nM
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BRAF
(cell-free assay)
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19 nM
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CRAF
(cell-free assay)
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56 nM
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MEK1
(cell-free assay)
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160 nM
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在HCT116 KRAS-突变型结肠直肠癌细胞中,CH5126766显著减少磷酸-MEK和磷酸-ERK的水平。CH5126766通过结合到MEK1抑制RAF激酶,并使MEK成为RAF的显性失活抑制剂。在Raf或RAS-突变型细胞系SK-MEL-28,SK-MEL-2,MIAPaCa-2,SW480,HCT116,和PC3细胞中,CH5126766抑制细胞生长,IC50分别为65,28,40,46,和277 nM。在含有BRAF V600E或NRAS突变型的两个黑色素瘤细胞系中,RO5126766诱导G1细胞周期阻滞,伴随CDK抑制剂p27上调,且细胞周期素D1下调。
在HCT116 (G13D KRAS)小鼠异种移植物模型中,CH5126766 (25 mg/kg, p.o.)抑制ERK信号输出,比标准MEK抑制剂更有效,其诱导MEK磷酸化,并且具有有效抗肿瘤活性。在HCT116 (K-ras)和COLO205 (B-raf)突变型异种移植物中,CH5126766 (0.3 mg/kg)引起[18 F]FDG摄取显著减少。在SK-MEL-2异种移植物模型中,RO5126766也会抑制肿瘤生长。
RO5126766(CH5126766)
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-18652 | Avutometinib | | 1 mg | 727元 |
2024/01/25 | HY-18652 | Avutometinib | | 5 mg | 1600元 |
RO5126766(CH5126766)
生产厂家
946128-88-7, RO5126766(CH5126766) 相关搜索:
- 合成有机化合物配体
- C21H18FN5O5S
- N-[3-氟-4-[[4-甲基-2-氧代-7-(2-嘧啶氧基)-2H-1-苯并吡喃-3-基]甲基]-2-吡啶]-N′-甲磺酰胺
- 化合物RO5126766
- 3-[2-[(甲氨基磺酰基)氨基]-3-氟吡啶-4-基]甲基]-4-甲基-7-[(嘧啶-2-基)氧]-2H-1-苯并吡喃-2-酮
- 946128-88-7
- Avutometinib
- MAPKK,CH 5126766,MEK,Ro 5126766,Raf kinases,Raf,Mitogen-activated protein kinase kinase,inhibit,Ro-5126766,CH-5126766,MAP2K,Inhibitor
- 3-[(2-((N-methylsulfamoyl)amino)-3-fluoropyridin-4-yl)methyl]-4-methyl-7-(pyrimidin-2-yloxy)-chromen-2-one,3-{2-(methylaminosulfonyl)amino-3-
- CH5126766
- Sulfamide, N-[3-fluoro-4-[[4-methyl-2-oxo-7-(2-pyrimidinyloxy)-2H-1-benzopyran-3-yl]methyl]-2-pyridinyl]-N'-methyl-
- 3-{2-(methylaminosulfonyl)amino-3-fluoropyridin-4-ylmethyl}-4-methyl-7-(pyrimidin-2-yloxy)-2-oxo-2H-1-benzopyran
- CS-1469
- 3-[[2-[(Methylaminosulfonyl)amino]-3-fluoropyridin-4-yl]methyl]-4-methyl-7-[(pyrimidin-2-yl)oxy]-2H-1-benzopyran-2-one
- RO5126766(CH5126766) 3-[[2-[(Methylaminosulfonyl)amino]-3-fluoropyridin-4-yl]methyl]-4-methyl-7-[(pyrimidin-2-yl)oxy]-2H-1-benzopyran-2-one
- RO5126766(CH5126766)