Description In vitro In vivo
ChemicalBook > CAS DataBase List > G-749

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
More
Less

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)
color 
White to off-white
More
Less

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.

More
Less

N-Bromosuccinimide Price

Cayman Chemical
Product number
22139
Product name
G-749
Purity
≥98%
Packaging
1mg
Price
$61
Updated
2024/03/01
Cayman Chemical
Product number
22139
Product name
G-749
Purity
≥98%
Packaging
5mg
Price
$207
Updated
2024/03/01
Cayman Chemical
Product number
22139
Product name
G-749
Purity
≥98%
Packaging
10mg
Price
$351
Updated
2024/03/01
Cayman Chemical
Product number
22139
Product name
G-749
Purity
≥98%
Packaging
25mg
Price
$656
Updated
2024/03/01
TRC
Product number
G110000
Product name
G-749
Packaging
1mg
Price
$140
Updated
2021/12/16
More
Less

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

More
Less

G-749 Suppliers

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Shanghai Kuanghao Chemistry Technology Co., Ltd.
Tel
13130049594 13130049594
Fax
021-37285512
Email
83219210@qq.com
Country
China
ProdList
95
Advantage
57
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
EnliPharma Technology Co., Ltd
Tel
0551-66399836 18955197623
Email
sales@enlipharma.com
Country
China
ProdList
1874
Advantage
55
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
CEG Chemical Science&Technology Co., Ltd.
Tel
Mobile:13665161512
Fax
+86-510-68873513
Country
China
ProdList
1785
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4456
Advantage
55
More
Less

View Lastest Price from G-749 manufacturers

Career Henan Chemical Co
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
Career Henan Chemical Co
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

1457983-28-6, G-749Related Search:


  • G-49
  • G-749 (Free base)
  • G-749
  • 8-Bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]pyrido[4,3-d]pyrimidin-5(6H)-one
  • 8-Bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]pyrido[4,3-d]pyrimidin-5(6H)-one G749
  • G-749, >=98%
  • 8-bromo-2-((1-methylpiperidin-4-yl)amino)-4-((4-phenoxyphenyl)amino)pyrido[4,3-d]pyrimidin-5(6H)-one
  • Pyrido[4,3-d]pyrimidin-5(6H)-one, 8-bromo-2-[(1-methyl-4-piperidinyl)amino]-4-[(4-phenoxyphenyl)amino]-
  • CS-1812
  • CS-3343
  • G-749; G749; G 749; CS-3343
  • G-749 USP/EP/BP
  • resistance,tyrosine,AML,G-749,FLT3,acute,kinase,myeloid,G 749,Cluster of differentiation antigen 135,inhibit,receptor,Inhibitor,leukemia,drug,Fms like tyrosine kinase 3,Fms-like,CD135,Apoptosis
  • Denfivontinib
  • 1457983-28-6
  • C25H25BrN6O2
  • Inhibitors
  • API