KB-0742 dihydrochloride
- CAS No.
- 2416874-75-2
- Chemical Name:
- KB-0742 dihydrochloride
- Synonyms
- KB-0742 dihydrochloride;KB0742,inhibit,CDK,CDK9,KB-0742,KB 0742,Ser7,Ser2,CRPC,KB 0742 dihydrochloride,antiproliferative,Cyclin dependent kinase,Ser5,oral,Inhibitor,KB0742 dihydrochloride,anticancer
- CBNumber:
- CB09624184
- Molecular Formula:
- C16H26ClN5
- Molecular Weight:
- 323.87
- MDL Number:
- MFCD32899897
- MOL File:
- 2416874-75-2.mol
KB-0742 dihydrochloride Chemical Properties,Uses,Production
Biological Activity
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity[1]. KB-0742 (6 hours; 0.1-10 μM; 22Rv1 cells) treatment significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5. Global androgen receptor (AR)-FL and AR-V protein levels are significantly reduced starting at 6 h treatment time, which is accompanied by the reduction of phospho-AR levels (Ser81)[1].KB-0742 (48-72 hours) treatment shows cytostatic effects in prostate cancer and leukemia cell lines. KB-0742 shows antiproliferative activity with GR50s of 0.183 μM and 0.288 μM for 22Rv1 cells and MV-4-11 AML cells, respectively[1].In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs[1]. 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].
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.
KB-0742 dihydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
KB-0742 dihydrochloride Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3423 | 58 |
| Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2989 | 58 |
| Chuzhou KeMail Chemical Technology Co., Ltd | 0550-5196001 15000891977 | wj520wjxby@126.com | China | 1836 | 55 |
| Shandong Jirun Biomedical Technology Co., Ltd. | 0539-0539-8613587 17661611089 | 2639273505@qq.com | China | 163 | 58 |
| Nantong Hi-Future Biotechnology Co., Ltd | 18051384581 | sales@chemhifuture.com | China | 3061 | 58 |