| Identification | Back Directory | [Name]
2-Butenamide, N-[4-[[(1R,3R)-3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]cyclohexyl]oxy]phenyl]-4-(dimethylamino)-, (2E)- | [CAS]
2227392-55-2 | [Synonyms]
BSJ-01-175
2-Butenamide, N-[4-[[(1R,3R)-3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]cyclohexyl]oxy]phenyl]-4-(dimethylamino)-, (2E)- | [Molecular Formula]
C30H33ClN6O2 | [MOL File]
2227392-55-2.mol | [Molecular Weight]
545.08 |
| Hazard Information | Back Directory | [Uses]
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]. | [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 |
| 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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| [IC 50]
CDK12; CDK13 | [References]
[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. DOI:10.1016/j.ejmech.2021.113481 |
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| Company Name: |
BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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