产品
编 号：F144578
分子式：C20H16ClN3O2
分子量：365.81
分子式：C20H16ClN3O2
分子量：365.81
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
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25mg
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询价
结构图
CAS No: 1380087-89-7
产品详情
生物活性：
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
体内研究：
Pelabresib (30-60 mg/kg; oral administration; for 28 days; MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals.Animal Model:MV-4-11 mouse xenograft model
Dosage:30 mg/kg once daily, 30 mg/kg twice daily, or 60 mg/kg once daily
Administration:Oral administration; for 28 days
Result:Suppressed of tumor growth, without any significant body weight loss in the animals.
体外研究：
Pelabresib (0-1500 nM; 72 hours; Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner.Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest.Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours.
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
体内研究：
Pelabresib (30-60 mg/kg; oral administration; for 28 days; MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals.Animal Model:MV-4-11 mouse xenograft model
Dosage:30 mg/kg once daily, 30 mg/kg twice daily, or 60 mg/kg once daily
Administration:Oral administration; for 28 days
Result:Suppressed of tumor growth, without any significant body weight loss in the animals.
体外研究：
Pelabresib (0-1500 nM; 72 hours; Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner.Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest.Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours.
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