1802175-07-0
1802175-07-0 结构式
基本信息
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-
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/12/22 | HY-109195 | Vebicorvir | 1802175-07-0 | 1 mg | 700元 |
| 2025/12/22 | HY-109195 | CPI-169 (R-enantioMer) Vebicorvir | 1802175-07-0 | 5mg | 1600元 |
| 2025/12/22 | HY-109195 | Vebicorvir | 1802175-07-0 | 10 mM * 1 mLin DMSO | 1645元 |
常见问题列表
|
EZH2 WT 0.24 nM (IC 50 ) |
EZH2 Y641N 0.51 nM (IC 50 ) |
EZH1 6.1 nM (IC 50 ) |
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.