1457983-28-6 Usage
Description
G-749 is a novel and potent FLT3 inhibitor with IC50 values ranging from 0.4 nM to 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, and shows lower potency against other tyrosine kinases. It is an inhibitor of Fms-like tyrosine receptor kinase 3 (FLT3) and has been found to inhibit the growth of human leukemia cell lines that express FLT3-ITD mutant kinase.
Uses
Used in Leukemia Treatment:
G-749 is used as an anticancer agent for the treatment of leukemia, particularly in cases where the cells express FLT3-ITD mutant kinase. It has demonstrated the ability to reduce tumor growth and increase survival in a dose-dependent manner in MV4-11 and Molm-14 murine leukemia xenograft models. Additionally, G-749 has shown more potent inhibition of bone marrow blasts derived from acute myeloid leukemia patients, especially those expressing the FLT3-ITD mutant receptor.
Used in Research and Development:
G-749 is used as a research tool for studying the role of FLT3 in various cellular processes and its potential as a therapeutic target in cancer treatment. Its potent inhibition of FLT3 makes it a valuable compound for investigating the underlying mechanisms of leukemia and other FLT3-driven diseases.
In vitro
In FLT3-WT-bearing RS4-11 cells and FLT3-ITD-harboring MV4-11 and Molm-14 cells, G-749 potently inhibits autophosphorylation of FLT3 with IC50 of ≤8 nM. In leukemia cells, G-749 shows antiproliferative activity by inducing apoptosis. In BaF3 cell lines that stably express FLT3-ITD/N676D, FLT3-ITD/F691L, FLT3-D835Y, or FLT3-D835Y/N676D, G-749 shows strong inhibitory activity with IC50 of <10 nM, and thus overcomes drug resistance. In blasts of AML patients, G-749 also exhibits potent antileukemia activity.
In vivo
In MV4-11 xenograft mice, G-749 (30 mg/kg p.o.) effectively inhibits the FLT3 pathway and significant inhibits tumor growth. In an orthogonal model of bone marrow engraftment using Molm-14 cells, G-749 (20 mg/kg p.o.) also inhibits tumor growth and increases survival.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1457983-28-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,5,7,9,8 and 3 respectively; the second part has 2 digits, 2 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 1457983-28:
(9*1)+(8*4)+(7*5)+(6*7)+(5*9)+(4*8)+(3*3)+(2*2)+(1*8)=216
216 % 10 = 6
So 1457983-28-6 is a valid CAS Registry Number.
