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JSH-150
😃Good
Catalog No. T8484Cas No. 2247481-21-4
JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.
JSH-150
😃Good
Purity: 99.96%
Catalog No. T8484Cas No. 2247481-21-4
JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $30 | In Stock | In Stock | |
| 5 mg | $89 | In Stock | In Stock | |
| 10 mg | $156 | In Stock | In Stock | |
| 25 mg | $347 | In Stock | In Stock | |
| 50 mg | $538 | In Stock | In Stock | |
| 100 mg | $651 | - | In Stock | |
| 500 mg | $1,390 | Backorder | Backorder |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.96%
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Product Introduction
Bioactivity
Chemical Properties
| Description | JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM. |
| Targets&IC50 | CDK14-CyclinY:1.68 μM, CDK1-CyclinB:1.34 μM, CDK5-p25:4.64 μM, CDK7-CyclinH-MNAT1:1.72 μM, CDK16-CyclinY:292 nM, CDK9-CyclinT1:1 nM, CDK2-CyclinA:2.86 μM |
| 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 |
| Smiles | COCCN[C@H]1CC[C@@H](CC1)Nc1cc(-c2csc(NCC3(CCOCC3)C#N)n2)c(Cl)cn1 |
| Relative Density. | 1.29 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
Storage & Solubility Information
| Storage | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (108.89 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.96 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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