CPI-169 (R-enantioMer)
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- CAS号:
- 1802175-07-0
- 英文名:
- CPI-169 (R-enantioMer)
- 英文别名:
- Vebicorvir;CPI-169 (R-enantioMer);CPI-169 (CPI 169 R-enantiomer);1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[(1R)-1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl-
- 中文名:
- CPI-169 (R-enantioMer)
- 中文别名:
- 化合物 T27069
- CBNumber:
- CB52715622
- 分子式:
- C27H36N4O5S
- 分子量:
- 528.66
- MOL File:
- 1802175-07-0.mol
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CPI-169 (R-enantioMer)化学性质
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密度:
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1.31±0.1 g/cm3(Predicted)
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酸度系数(pKa):
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11.01±0.10(Predicted)
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CPI-169 (R-enantioMer)性质、用途与生产工艺
CPI-169 (CPI 169 R-enantiomer) 是一种新颖的,有效的 EZH2 抑制剂,能够抑制 EZH2 WT,EZH2 Y641N 和 EZH1 的活性,IC50 值分别为 0.24 nM,0.51 nM 和 6.1 nM。
EZH2 WT
0.24 nM (IC
50
)
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EZH2 Y641N
0.51 nM (IC
50
)
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EZH1
6.1 nM (IC
50
)
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CPI-169 (CPI 169 R-enantiomer) inhibits the catalytic activity of PRC2 with an IC
50
of < 1nM, decreases cellular levels of H3K27me3 with an EC
50
of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI
50
of <5 μM.
CPI-169 (CPI 169 R-enantiomer) (200 mpk, s.c. BID) is well tolerated in mice with no observed toxic effect or body weight loss. CPI-169 treatment leads to tumor growth inhibition (TGI) of an EZH2 mutant KARPAS-422 DLBCL xenograft. CPI-169 (100 mpk, BID) with a single dose of CHOP leads tumors to rapidly regress and become unpalpable. In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects.
CPI-169 (R-enantioMer)
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 |
---|
2024/08/19 | HY-109195 | Vebicorvir | | 1 mg | 700元 |
2024/08/19 | HY-109195 | CPI-169 (R-enantioMer) Vebicorvir | 1802175-07-0 | 5mg | 1600元 |
CPI-169 (R-enantioMer)
生产厂家
1802175-07-0, CPI-169 (R-enantioMer) 相关搜索:
- 抑制剂
- 化合物 T27069
- 1802175-07-0
- Vebicorvir
- 1H-Indole-3-carboxamide, N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-1-[(1R)-1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl-
- CPI-169 (CPI 169 R-enantiomer)
- CPI-169 (R-enantioMer)