LY2784544 --- JAK2 inhibitor
Overview | |
Catalog # | bs-60079c-5mg-solid |
Product Name | LY2784544 --- JAK2 inhibitor |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 469.94 Formula: C23 H25 Cl F N7 O CAS Number: 1229236-86-5 InChi Key: SQSZANZGUXWJEA-UHFFFAOYSA-N InChi: InChI=1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30) Smiles: CC1C=C(NN=1)NC1C=C(CN2CCOCC2)C2=NC(C)=C(CC3C=CC(Cl)=CC=3F)N2N=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | LY2784544 is highly potent and selective mutant JAK2 (V617F) inhibitor with an IC50 of ~55 nM. It also inhibits IL-3-activated wild type JAK2 with an IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows anti-proliferative activity in JAK2 V617F-driven cells with an IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. LY2784544 significantly inhibits STAT5 phosphorylation in JAK2-V617F Ba/F3 xenografts. Currently LY2784544 is being investigated in a clinical trial for the treatment of essential thrombocythemia, polycythemia vera, and primary myelofibrosis. |