XL019

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F). Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma. XL019 is a potent, bioavailable JAK inhibitor with preference for JAK2 (IC50 = 2 nM) over JAK1 and JAK3 (IC50s = 130 and 250 nM, respectively). It is effective against JAK2V617F as well as JAK2 and inhibits phosphorylation of STAT5 in vivo.Formal Name: (2S)-N-[4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-2-pyrrolidinecarboxamide. CAS Number: 945755-56-6. Molecular Formula: C25H28N6O2. Formula Weight: 444.5. Purity: >90%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 300 nm. SMILES: O=C([C@H]1NCCC1)NC(C=C2)=CC=C2C3=CC=NC(NC(C=C4)=CC=C4N5CCOCC5)=N3. InChi Code: InChI=1S/C25H28N6O2/c32-24(23-2-1-12-26-23)28-19-5-3-18(4-6-19)22-11-13-27-25(30-22)29-20-7-9-21(10-8-20)31-14-16-33-17-15-31/h3-11,13,23,26H,1-2,12,14-17H2,(H,28,32)(H,27,29,30)/t23-/m0/s1. InChi Key: ISOCDPQFIXDIMS-QHCPKHFHSA-N.