Cat. No.: HY-119367

ODM-203

Customer Review

Based on 1 Customer Validation

ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC₅₀ values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment.

For research use only. We do not sell to patients.

Purity: 99.62%
CAS No.: 1430723-35-5
Formula: C₂₆H₂₁F₂N₅O₂S
Molecular Weight:505.54

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ODM-203 Chemical Structure

CAS No.: 1430723-35-5

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

FGFR1

11 nM (IC₅₀)

FGFR2

16 nM (IC₅₀)

FGFR3

6 nM (IC₅₀)

FGFR4

35 nM (IC₅₀)

VEGFR1

26 nM (IC₅₀)

VEGFR2

9 nM (IC₅₀)

VEGFR3

5 nM (IC₅₀)

DDR1

6 nM (IC₅₀)

RET

8 nM (IC₅₀)

SIK3

23 nM (IC₅₀)

PDGFRa

35 nM (IC₅₀)

MINK1

41 nM (IC₅₀)

MAP4K4

49 nM (IC₅₀)

All VEGFR Isoforms :

In Vitro

ODM-203 (eight-dose concentration series up to 3 μM; 96 h) potently inhibits FGFR signaling and proliferation in several FGFR-dependent cell lines^[1].
ODM-203 (eight-dose concentration series up to 3 μM; 10 days) inhibits endothelial tubule formation^[1].
ODM-203 (1, 10, 100, 1000 nM; 1 h) inhibiting FGFR and VEGFR cellular signaling in HUVEC cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

H1581 (ATCC-CRL-5878), SNU16 (ATCC-CRL-5974) and RT4 (HTB2) cells
Concentration:

Eight-dose concentration series up to 3 μM
Incubation Time:

96 h
Result:

Suppressed cell proliferation in a dose-dependent manner in H1581 (IC₅₀=104 nM), SNU16 (IC₅₀=132 nM) and RT4 cells (IC₅₀=192 nM).

Cell Viability Assay^[1]

Cell Line:

HUVECs and human umbilical vein endothelial cells (co-culture)
Concentration:

Eight-dose concentration series up to 3 μM
Incubation Time:

10 days (media and test agents were replaced every 2-3 days)
Result:

Inhibited endothelial tubule formation in a dose-dependent manner at non-toxic concentrations with an IC₅₀ value of 33 nM.

Western Blot Analysis^[1]

Cell Line:

HUVEC cells
Concentration:

1, 10, 100, 1000 nM
Incubation Time:

1 h
Result:

Suppressed both FGFR and VEGFR signaling.

In Vivo

ODM-203 (20, 40 mg/kg; p.o.; single daily for 21 days) inhibits FGFR phosphorylation and tumor growth in several FGFR-dependent xenografts by suppressing FGFR signaling in tumors^[1].
ODM-203 (7, 20, 40 mg/kg; p.o.; single daily for 21 days) shows strong anti-tumor activity in a VEGFR-dependent angiogenic orthotopic syngenic model (Renca) and suppresses angiogenesis^[1].
ODM-203 (20, 40 mg/kg; p.o.; single daily for 5 days) activates immune response in the tumor microenvironment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models)^[1].
Dosage:

20, 40 mg/kg
Administration:

Oral administration; single daily for 21 days.
Result:

Significantly inhibited tumour growth for 21 consecutive days.
Showed tumor growth inhibition (TGI) in RT4 xenografts was 37% and 92% with dosage of 20 and 40 mg/kg, respectively.

Animal Model:

Male balb/c mice (8-week-old; orthotopic renca syngenic model)^[1].
Dosage:

7, 20, 40 mg/kg
Administration:

Oral administration; single daily for 21 days.
Result:

Showed tumor growth inhibition were 39%, 58% and 75% for dosage of 7, 20 and 40 mg/kg, respectively.
Inhibited formation of lung metastasis, and suppressed angiogenesis.

Animal Model:

Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model)^[1].
Dosage:

20, 40 mg/kg
Administration:

Oral administration; single daily for 5 days.
Result:

Resulted in an increase in the percentage of total and CD4 T cells.
Decreased the expression of immune check points PD-1 and PD-L1 and increased IFN-γ expression on both CD8 T cells and NK cells.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1430723-35-5
Appearance Solid
Molecular Weight 505.54
Formula C₂₆H₂₁F₂N₅O₂S
Color White to yellow
SMILES

CN(N=C1)C=C1C2=CC=C3C(N=CN3C4=CC(C5=CC=C(F)C=C5F)=CC(NS(C6CC6)(=O)=O)=C4)=C2
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 66.67 mg/mL (131.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9781 mL

9.8904 mL

19.7808 mL

5 mM

0.3956 mL

1.9781 mL

3.9562 mL

10 mM

0.1978 mL

0.9890 mL

1.9781 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Holmström TH, et al. ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity. Mol Cancer Ther. 2019 Jan;18(1):28-38. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9781 mL	9.8904 mL	19.7808 mL	49.4521 mL
	5 mM	0.3956 mL	1.9781 mL	3.9562 mL	9.8904 mL
	10 mM	0.1978 mL	0.9890 mL	1.9781 mL	4.9452 mL
	15 mM	0.1319 mL	0.6594 mL	1.3187 mL	3.2968 mL
	20 mM	0.0989 mL	0.4945 mL	0.9890 mL	2.4726 mL
	25 mM	0.0791 mL	0.3956 mL	0.7912 mL	1.9781 mL
	30 mM	0.0659 mL	0.3297 mL	0.6594 mL	1.6484 mL
	40 mM	0.0495 mL	0.2473 mL	0.4945 mL	1.2363 mL
	50 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9890 mL
	60 mM	0.0330 mL	0.1648 mL	0.3297 mL	0.8242 mL
	80 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6182 mL
	100 mM	0.0198 mL	0.0989 mL	0.1978 mL	0.4945 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

ODM-203

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All VEGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ODM-203 Related Classifications

Cat. No.: HY-119367