BSJ-01-175

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BSJ-01-175 

BSJ-01-175 是一种有效的、选择性 CDK12/13 共价抑制剂。BSJ-01-175 表现出对癌细胞卓越的选择性、对磷酸化RNA 聚合酶 II 的有效抑制以及显著下调 CDK12 靶向基因。

BSJ-01-175

BSJ-01-175 Chemical Structure

CAS No. : 2227392-55-2

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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[1].

IC50 & Target

CDK12

 

CDK13

 

体外研究
(In Vitro)

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[1].
BSJ-01–175 (0-10 μM; 72 hours) slightly decreases the activity of TC71 Ewing sarcoma cells compared to THZ531[1].
BSJ-01–175 (0-5 μM) specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Kelly wild type or CDK12C1039F cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Observed a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039.

Cell Proliferation Assay[1]

Cell Line: TC71 Ewing sarcoma cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Slightly decreased the activity compared to THZ531.

体内研究
(In Vivo)

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[1].
Assessment of Pharmacokinetics (PK) profile of BSJ-01-175 in mouse[1].

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUClast (h•ng/mL) T1/2 (h) CL (mL/min/kg) VSS (L/kg) F (%)
IV 3 1511 1832 2.2 24.9 3.9
PO 10 2 272 1043 17

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (BALB/c, 7-8 weeks) bearing TC71 Ewing sarcoma cells[1]
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.

分子量

545.08

Formula

C30H33ClN6O2
CAS 号

2227392-55-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Jiang B, et al. Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma. Eur J Med Chem. 2021;221:113481.

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