DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
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.