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• 產品描述： 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)

• 靶點： IC50: 0.4 nM (FLT3-WT), 0.6 nM (FLT3-D835Y);Apoptosis;FLT;c-RET;TAMReceptor;AuroraKinase

• 體外研究：
  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.

• 體內研究：
  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.

• 參考文獻：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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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• pg ng μg mg g kg =
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