JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC 50 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
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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: PC-9, H1975 and PANC-1 cells Concentration: 6.3 μg/mL, 12.5 μg/mL, 25 μg/mL, 50 μg/mL Incubation Time: 48 hours Result: Exhibited significantly antiproliferative activity against all of these cancer cell lines.
Form:Solid
IC50& Target:JAK2 22.86 μg/mL (IC 50 )
Names and Identifiers
Canonical SMILES
O=C(C1=C(N)N=C(NC2=CC=CC=C2)S1)C3=CC=C(Cl)S3
Molecular Weight
335.83
Certificates
Certificate of Analysis(COA)
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Chemical and Physical Properties
Solubility
DMSO : 60 mg/mL (178.66 mM; ultrasonic and adjust pH to 5 with HCl)
