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
- Molecular Weight:
- 521.41
- MDL Number:
- MFCD28167815
- MOL File:
- 1457983-28-6.mol
- MSDS File:
- SDS
| 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) |
| FDA UNII | B06W426B66 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
G-749 price More Price(19)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22139 | G-749 ≥98% | 1457983-28-6 | 1mg | $61 | 2024-03-01 | Buy |
| Cayman Chemical | 22139 | G-749 ≥98% | 1457983-28-6 | 5mg | $207 | 2024-03-01 | Buy |
| Cayman Chemical | 22139 | G-749 ≥98% | 1457983-28-6 | 10mg | $351 | 2024-03-01 | Buy |
| Cayman Chemical | 22139 | G-749 ≥98% | 1457983-28-6 | 25mg | $656 | 2024-03-01 | Buy |
| TRC | G110000 | G-749 | 1457983-28-6 | 1mg | $140 | 2021-12-16 | Buy |
G-749 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29016 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
View Lastest Price from G-749 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
![Pyrido[4,?3-?d]?pyrimidin-?5(6H)?-?one, 8-?bromo-?2-?[(1-?methyl-?4-?piperidinyl)?amino]?-?4-?[(4-?phenoxyphenyl)?amino]?- pictures](https://img.chemicalbook.com/ProductImageEN/2019-12/Small/6071f2ba-f93d-486f-9cdb-74f52151c90f.png) |
2019-12-24 | Pyrido[4,?3-?d]?pyrimidin-?5(6H)?-?one, 8-?bromo-?2-?[(1-?methyl-?4-?piperidinyl)?amino]?-?4-?[(4-?phenoxyphenyl)?amino]?-
1457983-28-6
|
US $1.00 / KG | 1KG | Min98% HPLC | g/kg/ton | Career Henan Chemical Co | |
 |
2019-12-23 | NAPHTHOL AS-MX
92-75-1
|
US $1.00 / ASSAYS | 1ASSAYS | Min98% HPLC | 10t | Career Henan Chemical Co |
-
- Pyrido[4,?3-?d]?pyrimidin-?5(6H)?-?one, 8-?bromo-?2-?[(1-?methyl-?4-?piperidinyl)?amino]?-?4-?[(4-?phenoxyphenyl)?amino]?-
1457983-28-6
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co
-
- NAPHTHOL AS-MX
92-75-1
- US $1.00 / ASSAYS
- Min98% HPLC
- Career Henan Chemical Co