Denfivontinib_product_DataBase

Bioactivity

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 drug resistance for acute myeloid leukemia (AML)[1].

Target

IC50: 0.4 nM (FLT3-WT), 0.6 nM (FLT3-D835Y)

Invitro

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[1].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[1].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[1].Denfivontinib (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis[1].Denfivontinib (1.6-1000 nM; 2 hours) shows more potent inhibition of p-FLT3, p-ERK1/2, and p-AKT than AC220 and PKC412[1]. Cell Proliferation Assay[1] Cell Line:

In Vivo

Denfivontinib (3-30 mg/kg; p.o.; daily; for 28 days) shows effective antitumor activity in mouse models[1]. Animal Model:

Name

Denfivontinib

CAS

1457983-28-6

Formula

C25H25BrN6O2

Molar Mass

521.41

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Denfivontinib

CAS: 1457983-28-6 F: C25H25BrN6O2 W: 521.41