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2230974-62-4

2230974-62-4 Structure

2230974-62-4 Structure
IdentificationBack Directory
[Name]

2-Propenamide, N-[(3S,4S)-3-[[6-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(3-methoxy-3-methyl-1-azetidinyl)pyrido[3,4-d]pyrimidin-2-yl]amino]tetrahydro-2H-pyran-4-yl]-
[CAS]

2230974-62-4
[Synonyms]

2-Propenamide, N-[(3S,4S)-3-[[6-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(3-methoxy-3-methyl-1-azetidinyl)pyrido[3,4-d]pyrimidin-2-yl]amino]tetrahydro-2H-pyran-4-yl]-
[Molecular Formula]

C28H32F2N6O5
[MOL File]

2230974-62-4.mol
[Molecular Weight]

570.59
Chemical PropertiesBack Directory
[density ]

1.37±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

13.72±0.40(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model[1][2].
[in vivo]

ABSK-011 (oral) dose-dependently inhibits the growth of subcutaneous xenograft tumors with FGFR4 activity and induced tumor regression. Safety studies shows that ABSK-011 had no inhibitory effect on CYP family members, hERG, etc[1].

[References]

[1] Chen Z. Abstract LB-272: Discovery and characterization of a novel FGFR4 Inhibitor for the treatment of hepatocellular carcinoma[J]. Cancer Research, 2018, 78(13_Supplement): LB-272-LB-272.
[2] Zhang N, et al. Selective FGFR4 inhibitor Irpagratinib (ABSK011) exhibits broad synergistic and combinatory anti-tumor effects with other therapeutic agents in preclinical HCC models]. Cancer Research, 2024, 84(6_Supplement): 1228-1228.
Spectrum DetailBack Directory
[Spectrum Detail]

2-Propenamide, N-[(3S,4S)-3-[[6-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(3-methoxy-3-methyl-1-azetidinyl)pyrido[3,4-d]pyrimidin-2-yl]amino]tetrahydro-2H-pyran-4-yl]-(2230974-62-4)1HNMR
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