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LY 2784544
- Gandotinib
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H25ClFN7O
- MW: 469.94
Description
Potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase (IC50 value 20 and 55 nM for inhibition of JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells, respectively), with no significant inhibitory effect on IL-3 stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50 values >1180 nM) A selective tool for suppression of JAK2V617F-induced myeloproliferative neoplasm (MPN) pathogenesis while minimizing effects on hematopoietic progenitor cells. Moreover, LY2784544 induced apoptosis in inflammatory breast cancer spheres through targeting IL-6-JAK-STAT3 pathway; tested positive in Phase I study in patients with myelofibrosis (MF), polycythemia vera (PV), and essential thrombocythemia (ET).
More Information
| Parent CAS No. | 1229236-86-5 |
|---|---|
| Chemical Name | 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine |
| SMILES | C12=NC(C)=C(CC3=CC=C(Cl)C=C3F)N1N=C(NC1C=C(C)NN=1)C=C2CN1CCOCC1 |
| MFCD | N.A. |
| 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) |
| InChiKey | SQSZANZGUXWJEA-UHFFFAOYSA-N |
| CID | 46213929 |
| Short Description | JAK2 Inhibitor |
References
- L Ma et al. Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J. 2013 Apr; 3(4): e109.
- RA Mesa et al. Phase I study of LY2784544, a JAK2 selective inhibitor, in patients with myelofibrosis (MF), polycythemia vera (PV), and essential thrombocythemia (ET). Blood 122.21 (2013): 665-665.
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