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]-

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 list
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CAS:1628793-01-0
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CAS:1628793-01-0
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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

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  • $2180.00 / 50mg
  • 2026-01-05
  • CAS:1628793-01-0
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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]- Basic information
Product 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: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]-;FGFR4-IN-5;FGFR4 IN 5,FGFR-4-IN-5,FGFR4IN5;FGFR4-IN-2
CAS:1628793-01-0
MF:C23H23Cl2N5O5
MW:520.37
EINECS:
Product Categories:
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]- Structure
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
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
pka13.65±0.40(Predicted)
color White to off-white
Safety Information
MSDS Information
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]- Usage And Synthesis
UsesFGFR4-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].
Biological ActivityFGFR4-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].
in vivo

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].

Animal Model:Hep3B cell bearing mice model[1]
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; twice daily; 28 days
Result:Resulted in tumor regression and sustained growth inhibition.
Animal Model:Sorafenib-resistant tumors established to mice bearing Huh7 tumors[1]
Dosage:10, 30, and 100 mg/kg
Administration:Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result:Resulted in dose-dependent growth inhibition of resistant tumors.
IC 50FGFR4: 6.5 nM (IC50); FGFR2: 505 nM (IC50)
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
Tag: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]-(1628793-01-0) Related Product Information

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