G-749 (Synonyms: G-749) |
| Katalog-Nr.GC12178 |
G-749 ist ein potenter, oral aktiver und ATP-kompetitiver FLT3-Inhibitor mit IC50-Werten von 0,4 nM und 0,6 nM fÜr FLT3-Wildtyp bzw. FLT3-D835Y. G-749 kann fÜr die Erforschung von Arzneimittelresistenzen bei akuter myeloischer LeukÄmie (AML) verwendet werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1457983-28-6
Sample solution is provided at 25 µL, 10mM.
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G-749 is a selective inhibitor of Fms-like tyrosine receptor kinase-3 (FLT3) with IC50 value of 0.4 nM for wild-type FLT31.
G-749 is a synthesized and ATP-competitive inhibitor of wild-type FLT3 with high potency. It inhibited the autophosphorylation of FLT3 with IC50 value of ≤ 8 nM in RS4-11 leukemia cells. It also has inhibitory activity against various FLT3 mutants. In BaF3 cell lines that stably express FLT3-ITD/N676D, -ITD/F691L, -D835Y or -D835Y/N676D, G-749 showed strong potency against autophosphorylation of all tested FLT3 mutants with IC50 of < 10 nM. In MV4-11 and Molm-14 cell lines addicted to FLT3-ITD, G-749 significantly suppressed cell proliferation as well as increased active caspase 3/7 level and cleaved PARP in a dose-dependent manner. Besides that, G-749 showed high potency against p-FLT3, p-ERK1/2 and p-AKT even in high FLT3 ligand milieu1.
References:
1. Lee H K, Kim H W, Lee I Y, et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood, 2014, 123(14): 2209-2219.
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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