| Identification | Back Directory | [Name]
Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[4-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-1-yl]phenyl]-3-(trifluoromethyl)- | [CAS]
2479290-65-6 | [Synonyms]
CHMFL-48
Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[4-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-1-yl]phenyl]-3-(trifluoromethyl)- | [Molecular Formula]
C31H30F3N7O | [MOL File]
2479290-65-6.mol | [Molecular Weight]
573.61 |
| Hazard Information | Back Directory | [Uses]
CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML)[1]. | [IC 50]
WT BCR-ABL: 1 nM (IC50); Bcr-AblT315I: 0.8 nM (IC50); STAT5 | [References]
[1] Lu T, et al. Discovery of a highly potent kinase inhibitor capable of overcoming multiple imatinib-resistant ABL mutants for chronic myeloid leukemia (CML). Eur J Pharmacol. 2021 Apr 15;897:173944. DOI:10.1016/j.ejphar.2021.173944 |
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