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Background Information:
CYT387 (Momelotinib) is an ATP-competitive small molecule potently inhibiting JAK1/JAK2 kinases (IC50 = 11 and 18 nM, respectively), with significantly less activity against JAK3 (IC50 = 155 nM).
Reference:
1. Pardanani A, Lasho T, Smith G, Burns CJ, Fantino E, Tefferi A., CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients, Leukemia. 2009 Aug; 23(8):1441-5.
2. Tyner JW, Bumm TG, Deininger J, Wood L, Aichberger KJ, Loriaux MM, Druker BJ, Burns CJ, Fantino E, Deininger MW. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood. 2010 Jun 24; 115(25):5232-40.
APIM050134: CYT-387 (MOMELOTINIB)
CAS No.: 1056634-68-4.
Molecular Formula: C23H22N6O2.
Molecular Weight: 414.46.
Purity: >99.5% (HPLC at 220, 254 and 280 nM)).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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