Quizartinib [950769-58-1]

SYNkinase

Quizartinib [950769-58-1]

10

950769-58-1

Research Use Only

>95%

Warning

C29H32N6O4S

560.7

Chemical. CAS: 950769-58-1. Formula: C29H32N6O4S. MW: 560.7. Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in AML in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5microM, respectively, and has shown favorable activity and tolerability in phase I and II trials in acute myeloid leukemia, with QT prolongation as the dose-limiting toxicity. Recently, AC220 has also been shown to be an effective inhibitor of ATP-binding cassette (ABC) proteins ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein). Quizartinib inhibited transport of fluorescent ABCG2 and ABCB1 substrates in ABCG2- and ABCB1-overexpressing cells in a concentration-dependent manner, from 0.1 to 5microM and from 0.5 to 10microM, respectively, and inhibited-IAAP photolabeling of ABCG2 and ABCB1 with IC(50) values of 0.07 and 3.3microM, respectively. - Quizartinib (AC220) is a second-generation FLT3 inhibitor that has shown promising activity in AML in Phase II clinical trials. It inhibits mutant and wild-type FLT3 in vivo at 0.1 and 0.5microM, respectively, and has shown favorable activity and tolerability in phase I and II trials in acute myeloid leukemia, with QT prolongation as the dose-limiting toxicity. Recently, AC220 has also been shown to be an effective inhibitor of ATP-binding cassette (ABC) proteins ABCB1 (P-glycoprotein) and ABCG2 (breast cancer resistance protein). Quizartinib inhibited transport of fluorescent ABCG2 and ABCB1 substrates in ABCG2- and ABCB1-overexpressing cells in a concentration-dependent manner, from 0.1 to 5microM and from 0.5 to 10microM, respectively, and inhibited [125I]-IAAP photolabeling of ABCG2 and ABCB1 with IC(50) values of 0.07 and 3.3microM, respectively.

2°C to 8°C

51202000