KB-0742
- CAS No.
- 2416873-83-9
- Chemical Name:
- KB-0742
- Synonyms
- KB-0742;KB-0742 HCl;(1S,3S)-N1-(5-(Pentan-3-yl)pyrazolo[1,5-a]pyrimidin-7-yl)cyclopentane-1,3-diamine;1,3-Cyclopentanediamine, N1-[5-(1-ethylpropyl)pyrazolo[1,5-a]pyrimidin-7-yl]-, (1S,3S)-
- CBNumber:
- CB19273840
- Molecular Formula:
- C16H25N5
- Molecular Weight:
- 287.4
- MDL Number:
- MOL File:
- 2416873-83-9.mol
KB-0742 Chemical Properties,Uses,Production
Uses
KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity[1].
in vivo
KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models[1].
| Animal Model: | Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells[1] |
| Dosage: | 3 mg/kg, 10 mg/kg, and 30 mg/kg |
| Administration: | p.o.; daily; over 21 days |
| Result: | Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC). |
IC 50
CDK9/cyclinT1: 6 nM (IC50)
References
[1] André Richters, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol. 2020 Oct 20;S2451-9456(20)30380-9. DOI:10.1016/j.chembiol.2020.10.001
KB-0742 Preparation Products And Raw materials
Raw materials
Preparation Products
KB-0742 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 17702719238 | sales@sun-shinechem.com | China | 1015 | 64 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3466 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4601 | 55 | |
| Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2984 | 58 |
| ChengDu TongChuangYuan Pharmaceutical Co.Ltd | 028-83379370 13880556291 | tcy@tcypharm.com | China | 6293 | 58 |
| Shanghai Chaolan Chemical Technology Center | 021-QQ：65489617 15618227136 | Sales@ATKchemical.com | China | 9328 | 58 |
| Heze Development Zone chuangli Chemical Co., Ltd. | 0530-+86-530-529 6766，+86-15666160102 15666160102 | info@chuangli-chem.com | China | 839 | 55 |
| Shanghai Yu Ben Biotechnology Co., Ltd. | 15502154572 | yuben012@sina.com | China | 483 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9409 | 58 |