| Identification | Back Directory | [Name]
XL019 | [CAS]
945755-56-6 | [Synonyms]
XL019
XL019, >95%
XL019/XL-019
XL019, >=98%
XL019 USP/EP/BP
XL019; XL-019; XL 019.
(S)-N-(4-(2-(4-MORPHOLINOPHENYLAMINO)PYRIMIDIN-4-YL)PHENYL)PYRROLIDINE-2-CARBOXAMIDE
(2S)-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide
(2S)-N-[4-[2-[[4-(4-Morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-2-pyrrolidinecarboxamide
Pyrrolidine-2-carboxylic acid {4-[2-(4-morpholin-4-yl-phenylamino)-pyrimidin-4-yl]-phenyl}-amide
2-Pyrrolidinecarboxamide, N-[4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-, (2S)-
XL019 2-Pyrrolidinecarboxamide, N-[4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-, (2S)-
2S)-N-[4-[2-[[4-(4-Morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-2-pyrrolidinecarboxamide XL019 | [Molecular Formula]
C25H28N6O2 | [MDL Number]
MFCD24386874 | [MOL File]
945755-56-6.mol | [Molecular Weight]
444.529 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥11.125 mg/mL in DMSO | [form ]
solid | [color ]
Green to yellow |
| Hazard Information | Back Directory | [Uses]
XL019 is used in the synthesis of JAK-2 modulators for the treatment of related diseases.
| [Biological Activity]
XL019 is an ATP-binding site-targetingorally active JAK2 subtype-selective Janus kinase inhibitor (IC50 in nM = 2.2/JAK2 vs. 134.3/JAK1214.2/JAK3348.3/TYK2) with much reduced or little activity against 116 other kinases (IC50 in nM = 125.4/PDGFRB139.7/FLT3225.8/c-KIT313.8/p70S6K370/MLK1375.4/IKKbeta483.6/KDR546.7/PDGFRA554.5/FLT4910.5/FLT; IC50 >1 μM toward remaining 106 kinases)CYP (1A22C92D63A4 IC50 ≥20 μM)hERG (IC50 = 16 μM)and P-glycoprotein (IC50 >20 μM). XL019 effectively inhibits cellular STAT1/STAT3 phosphorylation both in HEL92.1.7 cultures (IC50 in nM = 386.4/pStat1 and 695/pStat3) and in HEL92.1.7 xenograft-derived tumor in mice in vivo (oral ED50 in mg/kg = 42/pStat1 and 210/pStat3) with significant HEL92.1.7 tumor suppression efficacy in mice (by 60% and 70% on day 14respectivelywith 200 and 300 mg/kg bid p.o. dosage). | [target]
JAK2 | [storage]
Store at -20°C |
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