产品
编 号：F750055
分子式：C30H33ClN6O2
分子量：545.08
分子式：C30H33ClN6O2
分子量：545.08
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2227392-55-2
产品详情
生物活性：
BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
体内研究：
BSJ-01–175 (10 mg/kg; i.p.; daily for 3 weeks) leads to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.Assessment of Pharmacokinetics (PK) profile of BSJ-01-175 in mouse.RouteDose (mg/kg)Tmax (h)Cmax (ng/mL)AUClast (h?ng/mL)T1/2 (h)CL (mL/min/kg)VSS (L/kg)F (%)
IV3151118322.224.93.9
PO102272104317
Animal Model:Female nude mice (BALB/c, 7-8 weeks) bearing TC71 Ewing sarcoma cells
Dosage:10 mg/kg
Administration:i.p.; daily for 3 weeks
Result:Led to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.
体外研究：
BSJ-01–175 (0-10 μM; 72 hours) causes a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039.BSJ-01–175 (0-10 μM; 72 hours) slightly decreases the activity of TC71 Ewing sarcoma cells compared to THZ531.BSJ-01–175 (0-5 μM) specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2.
BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.
体内研究：
BSJ-01–175 (10 mg/kg; i.p.; daily for 3 weeks) leads to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.Assessment of Pharmacokinetics (PK) profile of BSJ-01-175 in mouse.RouteDose (mg/kg)Tmax (h)Cmax (ng/mL)AUClast (h?ng/mL)T1/2 (h)CL (mL/min/kg)VSS (L/kg)F (%)
IV3151118322.224.93.9
PO102272104317
Animal Model:Female nude mice (BALB/c, 7-8 weeks) bearing TC71 Ewing sarcoma cells
Dosage:10 mg/kg
Administration:i.p.; daily for 3 weeks
Result:Led to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.
体外研究：
BSJ-01–175 (0-10 μM; 72 hours) causes a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039.BSJ-01–175 (0-10 μM; 72 hours) slightly decreases the activity of TC71 Ewing sarcoma cells compared to THZ531.BSJ-01–175 (0-5 μM) specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备