Home Angiogenesis FGFR inhibitor - VEGFR inhibitor ODM-203

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ODM-203 FGFR inhibitor

Cat.No.S8882

ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
ODM-203 FGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 505.54

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 505.54 Formula

C26H21F2N5O2S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1430723-35-5 -- Storage of Stock Solutions

Synonyms N/A Smiles CN1C=C(C=N1)C2=CC3=C(C=C2)N(C=N3)C4=CC(=CC(=C4)NS(=O)(=O)C5CC5)C6=C(C=C(C=C6)F)F

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (197.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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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
VEGFR3 [1]
(Cell-free assay)
5 nM
FGFR3 [1]
(Cell-free assay)
6 nM
VEGFR2 [1]
(Cell-free assay)
9 nM
FGFR1 [1]
(Cell-free assay)
11 nM
FGFR2 [1]
(Cell-free assay)
16 nM
VEGFR1 [1]
(Cell-free assay)
26 nM
FGFR4 [1]
(Cell-free assay)
35 nM
In vitro

In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines such as H1581,SNU16,and RT4 cells (IC50 50-150 nmol/L). [1]
In vivo

In vivo, ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses.[1]
References

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