G-749

ChemicalBook > CAS DataBase List > 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, 10 mM in DMSO;G-749; G749; G 749; CS-3343
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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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

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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

G-749, 10 mM in DMSO

1457983-28-6

C25H25BrN6O2

Inhibitors

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