Description In vitro In vivo
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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
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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
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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.

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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
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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

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G-749 Suppliers

China 77 France 1 India 1 United Kingdom 1 United States 11 Global 91
Alsachim SAS
Tel
--
Fax
--
Email
sales@alsachim.com
Country
France
ProdList
424
Advantage
0
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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:

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  • 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