Description
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.
Product information
CAS Number: 353512-04-6
Molecular Weight: 335.83
Formula: C14H10ClN3OS2
Chemical Name: 5-(5-chlorothiophene-2-carbonyl)-N2-phenyl-1,3-thiazole-2,4-diamine
Smiles: NC1N=C(NC2C=CC=CC=2)SC=1C(=O)C1=CC=C(Cl)S1
InChiKey: OFSYMZBCAABWIK-UHFFFAOYSA-N
InChi: InChI=1S/C14H10ClN3OS2/c15-10-7-6-9(20-10)11(19)12-13(16)18-14(21-12)17-8-4-2-1-3-5-8/h1-7H,16H2,(H,17,18)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
JAK2-IN-6 (Compound B2; 6.3-50 μg/mL; 48 hours; PC-9, H1975 and PANC-1 cells) treatment exhibits significantly antiproliferative activity against all of these cancer cell lines, with IC50 values of 18.1 μg/mL, 58.3 μg/mL, 40.6 μg/mL against PC-9, H1975 and PANC-1, respectively. JAK2-IN-6 (Compound B2), an intramolecular hydrogen bond is formed, holding the chlorothiophene substituent coplanar with the aminothiazole core. The chlorothiophene moiety is found to be located in the binding pocket adjacent to Val863 and Leu983, and extends towards the Asp994 of activation loop and the Gly993 of glycine-rich loop.
Products are for research use only. Not for human use.
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