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CAS NO.1229236-86-5
medical grade(1-50)Kilogrammedical grade(50-500)Kilogram
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Molecular Formula | C23H25ClFN7O |
Molar Mass | 469.94 |
Density | 1.45 |
Solubility | DMSO 94 mg/mL (200.02 mM); Water <1 mg/mL (<1 mM); Ethanol 9 mg/mL (19.15 mM) |
pKa | 14.12±0.10(Predicted) |
Storage Condition | -20℃ |
MDL | MFCD20482143 |
Use | A selective inhibitor of JAK2 mutant V617F. |
In vitro study | LY2784544 also inhibited IL-3-activated wild-type JAK2 with an IC50 of 2.26 µm. In the proliferation experiment, LY2784544 has anti-proliferative activity with an IC50 of 68 nM in cells driven by JAK2 V617F, while it has an IC50 of 1356 nM in cells driven by wild-type JAK2, when acting on jak3-driven cells, the IC50 was 940 nM. |
In vivo study | LY2784544 significantly inhibited STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts with a threshold effective dose 50 (TED50) of 12.7 mg/kg. LY2784544 acts on the MPN model induced by JAK2 V617F and also reduces the tumor burden V617F-GFP Ba/F3-JAK2, with a TED50 of 13.7 mg/kg after oral treatment. LY2784544 was orally applied to the spleen of SCID mice and had no effect on CD71/Ter119 positive erythroid progenitor cells. |