1. Protein Tyrosine Kinase/RTK
  2. FGFR

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
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50 mg USD 720 In-stock
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100 mg USD 1250 In-stock
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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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 cancer cells expressing different FGFR2 isoforms[1].

Alofanib (0.2, 0.4, 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: Alofanib inhibits growth of SKOV3 and HS578T cells with GI50s of 0.37 and 0.21 μM. Alofanib does 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].
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (302.37 mM; Need ultrasonic)

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

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Alofanib
Cat. No.:
HY-17601
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Alofanib

Cat. No.: HY-17601