JSH-150
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MedKoo CAT#: 573173

CAS#: 2247481-21-4

Description: JSH-150 is a potent CDK9 inhibitor. JSH-150 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). JSH-150displayed 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.


Price and Availability

Size Price Shipping out time Quantity
25mg USD 350 2 Weeks
50mg USD 650 2 Weeks
100mg USD 1050 2 Weeks
200mg USD 1650 2 Weeks
500mg USD 2450 2 Weeks
1g USD 3450 2 Weeks
2g USD 5450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-27. Prices are subject to change without notice.

JSH-150, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 573173
Name: JSH-150
CAS#: 2247481-21-4
Chemical Formula: C24H33ClN6O2S
Exact Mass: 504.2074
Molecular Weight: 505.08
Elemental Analysis: C, 57.07; H, 6.59; Cl, 7.02; N, 16.64; O, 6.34; S, 6.35


Synonym: JSH-150; JSH 150; JSH150;

IUPAC/Chemical Name: 4-(((4-(5-chloro-2-((4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile

InChi Key: XSDZPPRQLIZLDG-WEBLMRDCSA-N

InChi Code: InChI=1S/C24H33ClN6O2S/c1-32-11-8-27-17-2-4-18(5-3-17)30-22-12-19(20(25)13-28-22)21-14-34-23(31-21)29-16-24(15-26)6-9-33-10-7-24/h12-14,17-18,27H,2-11,16H2,1H3,(H,28,30)(H,29,31)/t17?,18-

SMILES Code: COCCNC1CC[C@H](NC2=NC=C(Cl)C(C3=CSC(NCC4(C#N)CCOCC4)=N3)=C2)CC1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

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 JSH-150 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.


References

1: Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q. 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. Eur J Med Chem. 2018 Oct 5;158:896-916. doi: 10.1016/j.ejmech.2018.09.025. Epub 2018 Sep 13. PubMed PMID: 30253346.