Alofanib (RPT835)

Catalog No.S8754 Batch:S875401

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Technical Data

Formula

C19H15N3O6S
Molecular Weight 413.40 CAS No. 1612888-66-0
Solubility (25°C)* In vitro DMSO 83 mg/mL (200.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
Targets
FGFR2 [1]
(Cell-free assay)
In vitro

Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2 in SKOV3 cell line. Cytotoxic effect of compound on ovarian cancer cells is low[1]. Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumour types (triple-negative breast cancer,melanoma, and ovarian cancer), alofanib inhibits FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose dependently inhibits the proliferation and migration of human and mouse endothelial cells (GI50: 11-58 nmol/l) compared with brivanib and bevacizumab[2].
In vivo

Intravenous alofanib significantly in dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. Alofanib suppresses angiogenesis in ovarian cancer mouse model[1]. In a FGFR-driven human tumour xenograft model, oral administration of alofanib is well tolerated and results in potent antitumour activity[2].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    SKOV3 cells

  • Concentrations

    0-1 μM

  • Incubation Time

    72 h

  • Method

    Cells were treated with alofanib (10, 100, and 1000 μM) for 72 h and whole-cell lysates were immunoblotted.
Animal Study:

[2]
  • Animal Models

    C57Bl/6 × DBA/2 F1 mice

  • Dosages

    15 mg/kg/d

  • Administration

    i.p.

Selleck's Alofanib (RPT835) has been cited by 5 publications

FGF7 enhances the expression of ACE2 in human islet organoids aggravating SARS-CoV-2 infection [ Signal Transduct Target Ther, 2024, 9(1):104] PubMed: 38654010
Paradoxical cancer cell proliferation after FGFR inhibition through decreased p21 signaling in FGFR1-amplified breast cancer cells [ Breast Cancer Res, 2024, 26(1):54] PubMed: 38553760
Endodermal BRD4 mediates epithelial-mesenchymal crosstalk during lung development [ bioRxiv, 2023, 10.1101/2023.05.21.541621] PubMed: none
Lenvatinib for effectively treating antiangiogenic drug-resistant nasopharyngeal carcinoma [ Cell Death Dis, 2022, 13(8):724] PubMed: 35985991
FGF-2 signaling in nasopharyngeal carcinoma modulates pericyte-macrophage crosstalk and metastasis [ JCI Insight, 2022, e157874] PubMed: 35439170

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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