G-749
Description In vitro In vivo- Product Name
- G-749
- CAS No.
- 1457983-28-6
- Chemical Name
- G-749
- Synonyms
- G-49;G-749;CS-3343;CS-1812;G-749, >=98%;Denfivontinib;G-749 USP/EP/BP;G-749 (Free base);G-749; G749; G 749; CS-3343;8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one
- CBNumber
- CB62715629
- Molecular Formula
- C25H25BrN6O2
- Formula Weight
- 521.41
- MOL File
- 1457983-28-6.mol
G-749 Property
- Density
- 1.487±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- ≥26.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
- form
- solid
- pka
- 8.32±0.40(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 22139
- Product name
- G-749
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $61
- Updated
- 2024/03/01
- Product number
- 22139
- Product name
- G-749
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $207
- Updated
- 2024/03/01
- Product number
- 22139
- Product name
- G-749
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $351
- Updated
- 2024/03/01
- Product number
- 22139
- Product name
- G-749
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $656
- Updated
- 2024/03/01
- Product number
- G110000
- Product name
- G-749
- Packaging
- 1mg
- Price
- $140
- Updated
- 2021/12/16
G-749 Chemical Properties,Usage,Production
Description
G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.
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.
Description
G-749 is an inhibitor of Fms-like tyrosine receptor kinase 3 (FLT3) with IC50 values ranging from 2.1 to 38.1 nM for wild-type and mutant (constitutively active) FLT3s in Ba/F3 cells expressing recombinant receptors. It also inhibits growth of human leukemia cell lines that express FLT3-ITD mutant kinase (IC50s = 3.5 and 7.5 nM for MV4-11 and Molm-14 cells, respectively) but has no effect on cells that lack FLT3 expression or that express wild-type FLT3. G-749 reduces tumor growth and increases survival in a dose-dependent manner in MV4-11 and Molm-14 murine leukemia xenograft models. It reduces growth of bone marrow blasts derived from acute myeloid leukemia patients, showing more potent inhibition of blasts expressing the FLT3-ITD mutant receptor.
Uses
G-749 is a potent FLT3 inhibitor. It shows lower potency against other tyrosine kinases.
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.
G-749 Preparation Products And Raw materials
Raw materials
Preparation Products
G-749 Suppliers
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View Lastest Price from G-749 manufacturers
- Product
- Pyrido[4,?3-?d]?pyrimidin-?5(6H)?-?one, 8-?bromo-?2-?[(1-?methyl-?4-?piperidinyl)?amino]?-?4-?[(4-?phenoxyphenyl)?amino]?- 1457983-28-6
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-23
- Product
- NAPHTHOL AS-MX 92-75-1
- Price
- US $1.00/ASSAYS
- Min. Order
- 1ASSAYS
- Purity
- Min98% HPLC
- Supply Ability
- 10t
- Release date
- 2019-12-20