WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407269
Description: JH-IX-179 is a novel type I ATP competitive, extremely potent and selective FLT3 inhibitor. JH-IX-179 has IC50 (FLT3, D835Y) = 4 nM; and IC50 (FLT3, ITD)=10nm. JH-IX-179 displays similar potency as crenolanib against FLT3-D835Y and FLT3-ITD transduced Ba/F3 cells as well as two human leukemia cell lines MOLM-13 and MOLM-14. However, JH-IX-179 is considerably more selective for FLT3 and FLT3 mutants than crenolanib. Furthermore, JH-IX-179 displayed very little human serum protein binding and effectively inhibited autophosphorylation of FLT3 and the activity of signaling molecules downstream of FLT3-D835Y and FLT3-ITD.
MedKoo Cat#: 407269
Chemical Formula: C26H24N6O
Exact Mass: 436.2012
Molecular Weight: 436.519
Elemental Analysis: C, 71.54; H, 5.54; N, 19.25; O, 3.67
Synonym: JH-IX-179; JH-IX 179; JH-IX179.
IUPAC/Chemical Name: 3-(1-(3-(dimethylamino)propyl)-1H-pyrazol-4-yl)-7-(1H-pyrazol-4-yl)indeno[1,2-b]indol-10(5H)-one
InChi Key: JRJKATLTRNXYCE-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H24N6O/c1-31(2)8-3-9-32-15-19(14-29-32)16-4-6-20-22(10-16)25-24(26(20)33)21-7-5-17(11-23(21)30-25)18-12-27-28-13-18/h4-7,10-15,30H,3,8-9H2,1-2H3,(H,27,28)
SMILES Code: O=C1C2=C(NC3=C2C=CC(C4=CNN=C4)=C3)C5=C1C=CC(C6=CN(CCCN(C)C)N=C6)=C5
Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor. John M. Hatcher, Ellen Weisberg, Taebo Sim, Richard M. Stone, Suiyang Liu, James D. Griffin, and Nathanael S. Gray. Publication Date (Web): March 8, 2016 (Letter). DOI: 10.1021/acsmedchemlett.5b00498