Rogaratinib

SKU: orb1706697

Description

Rogaratinib (BAY1163877) is a potent, selective, and orally bioavailable small molecule inhibitor targeting FGFR1, FGFR2, and FGFR3 kinase activity. It is widely used in preclinical research to investigate FGFR-driven pathologies, including in studies of cancer cell proliferation and tumor growth in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1443530-05-9
• MW: 466.56
• Purity: 99.61% (May vary between batches)
• Formula: C₂₃H₂₆N₆O₃S
• SMILES: COCc1c(CN2CCNC(=O)C2)n2ncnc(N)c2c1-c1cc2cc(C)cc(OC)c2s1
• Target: FGFR
• Solubility: DMSO:5.5 mg/mL (11.79 mM)

Bioactivity

• In Vitro:
  A novel pan-FGFR inhibitor, rogaratinib, in biochemical, cellular and in vivo efficacy studies in a variety of preclinical cancer models. In vitro kinase activity assays demonstrate that rogaratinib potently and selectively inhibits the activity of FGFRs 1, 2, 3 and 4. In line with this, rogaratinib reduced proliferation in FGFR-addicted cancer cell lines of various cancer types including lung, breast, colon and bladder cancer. FGFR and ERK phosphorylation interruption by rogaratinib treatment in several FGFR-amplified cell lines suggests that the anti-proliferative effects are mediated by FGFR/ERK pathway inhibition.
  Read more...

Storage & Handling

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

Alternative Names

BAY1163877, BAY-1163877, BAY 1163877, Inhibitor, FGFR4, FGFR3, FGFR2, FGFR, FGFR1, Fibroblast growth factor receptor, inhibit, Rogaratinib

Compound Identifiers

PubChem CID

71611869