1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Alofanib

Alofanib (Synonyms: RPT835)

Cat. No.: HY-17601 Purity: 99.83%
Handling Instructions

Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.

For research use only. We do not sell to patients.

Alofanib Chemical Structure

Alofanib Chemical Structure

CAS No. : 1612888-66-0

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10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
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50 mg USD 720 In-stock
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100 mg USD 1250 In-stock
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Description

Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity[1][2].

IC50 & Target

FGFR2

 

In Vitro

Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in hFOB and SUM 52PE cells expressing different FGFR2 isoforms[1].

Alofanib (0.2-0.8 μM, 6 hours) inhibits FGF-mediated proliferation in a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer) with GI50s of 16-370 nM[1].

Cell Proliferation Assay[1]

Cell Line: SKOV3, HS478T, Mel Kor cells
Concentration: 0.2, 0.4, 0.8 μM
Incubation Time: 6 hours after dosing, FGF2 is added at a concentration of 25 ng/ml
Result: Inhibited growth of SKOV3 and HS578T cells with GI50s of 0.37 and 0.21 μM. Did not potently inhibit growth of Mel Kor cells that do not contain FGFR2 (GI50>10 μM)[1].
In Vivo

In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg, gavage, daily, 40 days, N=10) is well tolerated and results in potent antitumour activity[1].

Treatment with alofanib (10 mg/kg/d, 0, 3 and 6 d, intraperitoneally) ablates experimental FGF-induced angiogenesis in vivo[1].

Animal Model: C57Bl/6 × DBA/2 F1 mice of 22–30 g[1]
Dosage: 10 mg/kg/d
Administration: Intraperitoneally, 0, 3 and 6 d
Result: Alofanib inhibits angiogenesis in mouse models[1].
Molecular Weight

413.40

Formula

C₁₉H₁₅N₃O₆S

CAS No.

1612888-66-0

SMILES

O=C(O)C1=CC=CC(S(=O)(NC2=CC(C3=CC=CN=C3)=C(C)C=C2[N+]([O-])=O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30.1 mg/mL (72.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4190 mL 12.0948 mL 24.1896 mL
5 mM 0.4838 mL 2.4190 mL 4.8379 mL
10 mM 0.2419 mL 1.2095 mL 2.4190 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Alofanib
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