2. Protein Tyrosine Kinase/RTK
  3. FGFR VEGFR
  4. ODM-203

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.

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ODM-203 Chemical Structure

ODM-203 Chemical Structure

CAS No. : 1430723-35-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

ODM-203 Related Antibodies

Top Publications Citing Use of Products

View All FGFR Isoform Specific Products:

View All Isoforms
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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)

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.

ODM-203 Related Antibodies

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
Molecular Weight

505.54

Formula

C26H21F2N5O2S
CAS No.
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9781 mL 9.8904 mL 19.7808 mL
5 mM 0.3956 mL 1.9781 mL 3.9562 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

SDS (252 KB)

COA (254 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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ODM-203 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ODM-2031430723-35-5ODM203ODM 203FGFRVEGFRFibroblast growth factor receptorVascular endothelial growth factor receptorcancerH1581SNU16RT4HUVECanti-tumor immunityInhibitorinhibitorinhibit

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