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JSH-150

Cat. No. M9558
JSH-150 Structure
Size Price Availability Quantity
5mg USD 110  USD110 In stock
10mg USD 190  USD190 In stock
25mg USD 420  USD420 In stock
50mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

JSH-150 is a potent CDK9 inhibitor with IC50 of 1 nM. JSH-150 exhibits potent antiproliferative activities in solid tumor cell lines such as A375 (melanoma), A431 (squamous), BE(2)M17 (neuroblastoma), GIST-T1 (GIST) and COLO205 (colon cancer) with GI50 values from 0.002 to 0.044 µM. In vivo, JSH-150 exhibits acceptable bioavailability in mice, rats and dogs (F=45.01%, 45.10% and 39.15%, respectively).

Chemical Information
Molecular Weight 505.08
Formula C24H33ClN6O2S
CAS Number 2247481-21-4
Solubility (25°C) DMSO ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Beilei Wang, et al. Eur J Med Chem. Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a Novel Highly Selective and Potent CDK9 Kinase Inhibitor

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  Catalog
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Keywords: JSH-150 supplier, CDK, inhibitors, activators


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