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Alofanib (RPT835) (Synonyms: RPT835)

Catalog No.GC32127

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

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Alofanib (RPT835) Chemical Structure

Cas No.: 1612888-66-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$89.00
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5mg
$81.00
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10mg
$117.00
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25mg
$234.00
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50mg
$351.00
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100mg
$540.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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

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 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].

[1]. Tsimafeyeu I, et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8. [2]. Khochenkov DA, et al. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7.

Chemical Properties

Cas No. 1612888-66-0 SDF
Synonyms RPT835
Canonical SMILES O=C(O)C1=CC=CC(S(=O)(NC2=CC(C3=CC=CN=C3)=C(C)C=C2[N+]([O-])=O)=O)=C1
Formula C19H15N3O6S M.Wt 413.4
Solubility DMSO : ≥ 30.1 mg/mL (72.81 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.419 mL 12.0948 mL 24.1896 mL
5 mM 0.4838 mL 2.419 mL 4.8379 mL
10 mM 0.2419 mL 1.2095 mL 2.419 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Reviews

Review for Alofanib (RPT835)

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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