WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407950
Description: CCT241736 is a potent and orally active and dual FLT3-Aurora inhibitor. CCT241736 has IC50 values against FLT3, Aurora A and Aurora B of 0.035, 0.015 and 0.1 μM respectively. CCT241736 inhibits a wide range of FLT3 mutants, including FLT3-ITD, -D835Y, -D835H, -K663Q and -N841I. In cellular assays, CCT241736 inhibits viability of the human FLT3-ITD positive AML cell lines MOLM-13 and MV-4;11 with EC50 values of 0.1 and 0.27
MedKoo Cat#: 407950
Chemical Formula: C22H23Cl2N7
Exact Mass: 455.1392
Molecular Weight: 456.375
Elemental Analysis: C, 57.90; H, 5.08; Cl, 15.54; N, 21.48
Synonym: CCT241736; CCT-241736; CCT 241736;
IUPAC/Chemical Name: 6-chloro-7-[4-[(4-chlorophenyl)methyl]-1-piperazinyl]-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine
InChi Key: AKJBLKUZXRMECW-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H23Cl2N7/c1-14-17(13-29(2)28-14)21-26-19-20(18(24)11-25-22(19)27-21)31-9-7-30(8-10-31)12-15-3-5-16(23)6-4-15/h3-6,11,13H,7-10,12H2,1-2H3,(H,25,26,27)
SMILES Code: CC1=NN(C)C=C1C2=NC3=C(N4CCN(CC5=CC=C(Cl)C=C5)CC4)C(Cl)=CN=C3N2
M respectively. In vivo, mouse tumor xenograft models of MOLM-13, MV-4;11 and the doubly-mutated cell line, MOLM-13-RES, are also sensitive to CCT241736, with biomarker modulation consistent with dual inhibition of FLT3 and Aurora kinases. In summary, dual inhibition of FLT3 and the critical mitotic kinase Aurora by CCT241736 may represent a novel treatment strategy for FLT3-mutated AML by overcoming the effects of high FL levels and limiting resistance caused by secondary mutations of the FLT3 gene.