Resigratinib

• Description:

  Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M) . Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer) [1][2].

• Product Name Alternative:

  KIN-3248

• UNSPSC:

  12352005

• Target:

  FGFR

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/resigratinib.html

• Purity:

  99.53

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  CNC1=C(C(N)=O)C(C#CC2=C(F)C=C(N(C3CC3)C=N4)C4=C2F)=NN1[C@H]5C[C@@H](N(C5)C(C=C)=O)COC

• Molecular Formula:

  C26H27F2N7O3

• Molecular Weight:

  523.53

• References & Citations:

  [1]Tyhonas JS, et al. Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations. J Med Chem. 2024 Feb 8;67 (3) :1734-1746.|[2]Balasooriya ER, et al. The Irreversible FGFR Inhibitor KIN-3248 Overcomes FGFR2 Kinase Domain Mutations. Clin Cancer Res. 2024 May 15;30 (10) :2181-2192.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 1

• CAS Number:

  [2750709-91-0]