Irpagratinib

SKU: orb2277624

Description

Irpagratinib (ABSK011) is a potent and orally bioavailable FGFR4 inhibitor that suppresses autophosphorylation and downstream signaling. It demonstrates antitumor activity in preclinical models and is used in research targeting cancers, particularly hepatocellular carcinoma and other gastrointestinal malignancies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2230974-62-4
• MW: 570.59
• Purity: 99.38% (May vary between batches)
• Formula: C₂₈H₃₂F₂N₆O₅
• SMILES: N(C1=NC=2C(=NC(=CC2C=N1)C3=C(F)C(OC)=CC(OC)=C3F)N4CC(OC)(C)C4)[C@H]5[C@@H](NC(C=C)=O)CCOC5
• Target: FGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.78 mM);DMSO:80 mg/mL (140.21 mM)

Bioactivity

• Target IC50:
  FGFR4:< 10 nM
• In Vivo:
  Oral Irpagratinib strongly inhibited the growth of subcutaneous xenograft tumors dependent on FGFR4 activity and induced their regression.
• In Vitro:
  Irpagratinib inhibits FGFR4 with IC50 < 10 nM and shows at least 50-fold selectivity against other FGFR kinases. Irpagratinib has the ability to irreversibly modify Cys552.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ABSK 011, ABSK011

Compound Identifiers

PubChem CID

135181440