Alofanib | B3009

Alofanib is a novel selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2) tyrosine kinase. It inhibits phosphorylation of FGF receptor substrate 2α (FRS2α) with IC₅₀ values of 7 nM and 9 nM in cancer cells expressing different FGFR2 isoforms. It inhibits FGF-mediated proliferation in a panel of four cell lines representing tumor types such as triple-negative breast cancer, melanoma, and ovarian cancer with 50% growth inhibition (GI₅₀) values of 16 nM-370 nM. It inhibits the proliferation and migration of human and mouse endothelial cells. It ablates experimental FGF-induced angiogenesis in vivo. Oral administration of alofanib shows potent antitumor activity in a FGFR-driven human tumor xenograft model.

Alofanib is a novel selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2) tyrosine kinase. It inhibits phosphorylation of FGF receptor substrate 2α (FRS2α) with IC₅₀ values of 7 nM and 9 nM in cancer cells expressing different FGFR2 isoforms. It inhibits FGF-mediated proliferation in a panel of four cell lines representing tumor types such as triple-negative breast cancer, melanoma, and ovarian cancer with 50% growth inhibition (GI₅₀) values of 16 nM-370 nM. It inhibits the proliferation and migration of human and mouse endothelial cells. It ablates experimental FGF-induced angiogenesis in vivo. Oral administration of alofanib shows potent antitumor activity in a FGFR-driven human tumor xenograft model.

B3009 | Alofanib DataSheet

Alternate Name/Synonyms: RPT835; 3-[(4-methyl-2-nitro-5-pyridin-3-ylphenyl)sulfamoyl]benzoic acid; Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-

Appearance: Yellow Solid

Formulation:

CAS Number: 1612888-66-0

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₁₉H₁₅N₃O₆S

Molecular Weight: 413.4

Cell-Permeable?: TRUE

Purity: >98%

Solubilities: ~30 mg/ml in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A novel selective allosteric inhibitor of FGFR2

MDL Number: MFCD30747921

PubChem CID: 86280646

SMILES: CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]

InChi: InChI=1S/C19H15N3O6S/c1-12-8-18(22(25)26)17(10-16(12)14-5-3-7-20-11-14)21-29(27,28)15-6-2-4-13(9-15)19(23)24/h2-11,21H,1H3,(H,23,24)

InChi Key: QUQGQIASFYWKAB-UHFFFAOYSA-N