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Alofanib (RPT835) FGFR inhibitor

Name: Alofanib (RPT835)
Brand: Selleck Chemicals
SKU: S8754
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8754

Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 with a dramatic inhibitory effect (IC50 <10 nM) on FGF2-induced phosphorylation 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.

Chemical Structure

Molecular Weight: 413.40

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S875401 DMSO]83 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.76%

99.76

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Chemical Information, Storage & Stability

Molecular Weight	413.40	Formula	C₁₉H₁₅N₃O₆S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1612888-66-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (200.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.09mM)	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 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.09mM)	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	FGFR2 ^[1] (Cell-free assay)
In vitro	Alofanib (RPT835) induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2 in SKOV3 cell line. Cytotoxic effect of this compound on ovarian cancer cells is low^[1]. It 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. This compound 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 (RPT835) significantly in dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. It suppresses angiogenesis in ovarian cancer mouse model^[1]. In a FGFR-driven human tumour xenograft model, oral administration of this compound is well tolerated and results in potent antitumour activity^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/27812884/ [2] https://pubmed.ncbi.nlm.nih.gov/27136102/

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