S80368 |
G-749 |
| 源叶(MedMol) | 98% |
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- 产品描述： Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML)
- 靶点： IC50: 0.4 nM (FLT3-WT), 0.6 nM (FLT3-D835Y)
- 体外研究：
Denfivontinib shows potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. Denfivontinib inhibits autophosphorylation of FLT3 with an IC50 value of ≤8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells. Denfivontinib (0.0001-10 nM; 72 hours) shows strong antiproliferation of leukemia cells addicted to FLT3-ITD (MV4-11 and Molm-14) in a dose-dependent manner. Denfivontinib (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis. Denfivontinib (1.6-1000 nM; 2 hours) shows more potent inhibition of p-FLT3, p-ERK1/2, and p-AKT than AC220 and PKC412. Cell Proliferation Assay Cell Line: MV4-11 cells, Molm-14 cells, K562 cells, HEL cells, RS4-11 cells Concentration: 0.0001-10 nM Incubation Time: 72 hours Result: Had antiproliferative activity for leukemia cells addicted to FLT3-ITD.Apoptosis Analysis Cell Line: MV4-11 cells Concentration: 25 nM, 50 nM, 100 nM Incubation Time: 36 hours Result: Increased apoptosis of MV4-11 cells in a dose-dependent manner. Western Blot Analysis Cell Line: Molm-14 cells Concentration: 1.6 nM, 80 nM, 40 nM, 200 nM, 1000 nM Incubation Time: 2 hours Result: Inhibited the phosphorylation of downstream effectors in the FLT3 signaling pathway, such as p-STAT5, p-AKT, p-ERK1/2, and p-FoxO3a.
- 体内研究：
Denfivontinib (3-30 mg/kg; p.o.; daily; for 28 days) shows effective antitumor activity in mouse models. Animal Model: Athymic nu/nu mice, subcutaneous MV4-11 xenograft mice Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Oral administration, daily, for 28 days Result: Suppressed tumor growth.
- 参考文献：
1. Lee HK, et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.918 ml 9.589 ml 19.179 ml 5 mM 0.384 ml 1.918 ml 3.836 ml 10 mM 0.192 ml 0.959 ml 1.918 ml 50 mM 0.038 ml 0.192 ml 0.384 ml
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