LY2784544

LY2784544

Biochem/physiol Actions

LY2784544 is an orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 µM/JAK2, 19.8 nM/20 µM/JAK1, 48.0 nM/2 µM/JAK3) with little activity toward 79 other kinases. LY2784544 selectively inhibits signaling/proliferation driven by oncogenic JAK2V617F (IC50 = 20/55 nM) over those mediated by wt JAK2 upon IL-3 induction (IC50 = 1183/1309 nM) in Ba/F3 cultures and displays in vivo efficacious in a JAK2V617F-induced murine MPN model (10-80 mg/kg bid po.). LY2784544 is also reported to display Zn-dependent (optimal [Zn+2] = 100 µM) GPR39 agonist activity, but not 11 other GPRs.

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Code Description Colour Manufacturer Composition Storage Temp. Solubility Form Assay Price Quantity
3576506 LY2784544 white to beige SIGMA-ALDRICH H2O, 0-4 mol/mol (moles per mole of product) 2-8°C
£580.82 (exc VAT) per 25MG
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3576507 LY2784544 white to beige SIGMA-ALDRICH H2O, 0-4 mol/mol (moles per mole of product) 2-8°C
£181.07 (exc VAT) per 5MG
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