2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]-
- CAS No.
- 1628793-01-0
- Chemical Name:
- 2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]-
- Synonyms
- FGFR4-IN-5;FGFR4-IN-2;FGFR4 IN 5,FGFR-4-IN-5,FGFR4IN5;2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]-
- CBNumber:
- CB79276409
- Molecular Formula:
- C23H23Cl2N5O5
- Molecular Weight:
- 520.37
- MDL Number:
- MFCD34470864
- MOL File:
- 1628793-01-0.mol
2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]- Properties
Density | 1.47±0.1 g/cm3(Predicted) |
---|---|
storage temp. | Store at -20°C |
solubility | DMSO : 100 mg/mL (192.17 mM; Need ultrasonic) |
form | Solid |
pka | 13.65±0.40(Predicted) |
color | White to off-white |
2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]- Chemical Properties,Uses,Production
Biological Activity
FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research[1]. FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high Cmax, low clearance, the Cmax values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively[1].FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model[1].FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %δT/δC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo[1].
References
[1]. Haibo Liu, et al. Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma. ACS Med Chem Lett. 2020 Mar 6;11(10):1899-1904.
2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38631 | 58 | |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52924 | 58 |
NanJing Xienuo bio Co.,Ltd. | 025-84112752 13805181430 | 154301870@qq.com | China | 1000 | 55 |
Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11974 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19704 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
Aladdin Scientific | 58 |
NanJing Xienuo bio Co.,Ltd. | 55 |
Shanghai Yifei Biotechnology Co. , Ltd. | 58 |
TargetMol Chemicals Inc. | 58 |
View Lastest Price from 2-Propenamide, N-[(3R,4S)-4-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)-7,8-dihydro-8-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl]amino]tetrahydro-3-furanyl]- manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2024-10-28 | FGFR4-IN-5
1628793-01-0
|
US $2180.00-1670.00 / mg | 10g | TargetMol Chemicals Inc. |
- FGFR4-IN-5
1628793-01-0
- US $2180.00-1670.00 / mg
- TargetMol Chemicals Inc.