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。
| 生物活性 | BSJ-01-175 is a potent and selectiveCDK12/13covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes incancercells[1]. |
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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].
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. |
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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(hong/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 |
| 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. |
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| 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. |
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