KB-0742 dihydrochloride
- Product Name
- KB-0742 dihydrochloride
- CAS No.
- 2416874-75-2
- Chemical Name
- KB-0742 dihydrochloride
- Synonyms
- KB-0742 dihydrochloride;KB-0742 dihydrochloride, 10 mM in DMSO;(1S,3S)-N1-(5-(Pentan-3-yl)pyrazolo[1,5-a]pyrimidin-7-yl)cyclopentane-1,3-diamine 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
- Formula Weight
- 323.87
- MOL File
- 2416874-75-2.mol
KB-0742 dihydrochloride Property
- storage temp.
- 4°C, away from moisture
- solubility
- |DMSO : 62.5 mg/mL (173.45 mM; Need ultrasonic)
- form
- Solid
- color
- Light yellow to yellow
- Water Solubility
- Water : 100 mg/mL (277.52 mM; Need ultrasonic)
KB-0742 dihydrochloride Chemical Properties,Usage,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
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