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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
5 mg | $89 | In Stock | |
10 mg | $156 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $538 | In Stock | |
100 mg | $651 | In Stock | |
500 mg | $1,390 | In Stock |
Description | JSH-150 is a highly selective CDK9 inhibitor(IC50 : 1 nM). |
In vitro | A highly selective inhibitor compound 40 (JSH-150), which exhibited an IC50 of 1 nM against CDK9 kinase in the biochemical assay and achieved around 300 10000-fold selectivity over other CDK kinase family members.?In addition, it also displayed high selectivity over other 468 kinases/mutants (KINOMEscan S score(1) = 0.01).Compound 40 displayed potent antiproliferative effects against melanoma, neuroblastoma, hepatoma, colon cancer, lung cancer as well as leukemia cell lines.?It could dose-dependently inhibit the phosphorylation of RNA Pol II, suppress the expression of MCL-1 and c-Myc, arrest the cell cycle and induce the apoptosis in the leukemia cells. |
In vivo | In the MV4-11 cell-inoculated xenograft mouse model, 10 mg/kg dosage of 40 could almost completely suppress the tumor progression.?The high selectivity and good in vivo PK/PD profile suggested that 40 would be a good pharmacological tool to study CDK9-mediated physiology and pathology as well as a potential drug candidate for leukemia and other cancers. |
Molecular Weight | 505.08 |
Formula | C24H33ClN6O2S |
Cas No. | 2247481-21-4 |
Storage | keep away from direct sunlight,store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (108.89 mM) ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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