G-749 (Synonyms: G-749) |
| رقم الكتالوجGC12178 |
G-749 هو مثبط FLT3 فعال عن طريق الفم و ATP تنافسي ، مع IC50s من 0.4 نانومتر و 0.6 نانومتر للنوع البري FLT3 و FLT3-D835Y ، على التوالييمكن استخدام G-749 في البحث عن مقاومة الأدوية لسرطان الدم النخاعي الحاد (AML)
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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.
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