An allosteric inhibitor of FGFR2
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Alofanib

Item No. 31754

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[4-methyl-2-nitro-5-(3-pyridinyl)phenyl]amino]sulfonyl]-benzoic acid
CAS Number
1612888-66-0
Synonyms
  • RPT835
Molecular Formula
C19H15N3O6S
Formula Weight
413.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/mlPBS (pH 7.2): slightly soluble
SMILES
O=C(C1=CC=CC(S(=O)(NC2=C([N+]([O-])=O)C=C(C)C(C3=CN=CC=C3)=C2)=O)=C1)O
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $95

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    25 mg

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    50 mg

    $370

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    100 mg

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    Product Description

    Alofanib is an allosteric inhibitor of FGFR2.1,2 It inhibits FGF2-induced phosphorylation of FGFR substrate 2 (FRS2α) in KATO III gastric carcinoma cells (IC50 = <10 nM).2 Alofanib inhibits the growth of SKOV3 ovarian and Hs 578T breast cancer cells (GI50s = 370 and 210 nM, respectively). It inhibits proliferation of human umbilical vein endothelial cells (HUVECs) induced by basic FGF (bFGF; IC50 = 11 nM) and tube formation of SVEC4-10 endothelial cells when used at a concentration of 50 nM.1 It also inhibits migration of SVEC4-10 cells in a wound healing assay. Alofanib (50 mg/kg) decreases the number of microvessels in tumor tissue by 50% in a SKOV3 ovarian serous carcinoma mouse model. It reduces tumor growth in mouse xenograft models when administered at a dose of 30 mg/kg per day, and the degree of tumor volume reduction positively correlates with the expression level of FGFR22

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Khochenkov, D.A., Solomko, E.S., Peretolchina, N.M., et al. Antiangiogenic activity of alofanib, an allosteric inhibitor of fibroblast growth factor receptor 2. Bull. Exp. Biol. Med. 160(1), 84-87 (2015).

    2. Tsimafeyeu, I., Ludes-Meyers, J., Stepanova, E., et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur. J. Cancer 61, 20-28 (2016).