| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
FGFR1 (IC50 = 11 nM); FGFR2 (IC50 = 16 nM); FGFR3 (IC50 = 6 nM); FGFR4 (IC50 = 35 nM); VEGFR1 (IC50 = 26 nM); VEGFR2 (IC50 = 9 nM); VEGFR3 (IC50 = 5 nM); DDR1 (IC50 = 6 nM); RET (IC50 = 8 nM); SIK3 (IC50 = 23 nM); PDGFRa (IC50 = 35 nM); MINK1 (IC50 = 41 nM); MAP4K4 (IC50 = 49 nM)
The primary targets of ODM-203 are FGFR (fibroblast growth factor receptor) and VEGFR (vascular endothelial growth factor receptor) families. It acts as a potent inhibitor of both receptor families. By inhibiting VEGFR and FGFR, it blocks angiogenesis and tumor cell proliferation signaling pathways. It also inhibits PDGFRα with an IC50 of 35 nM. |
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| ln Vitro |
ODM-203 exhibits a comparable level of potency in suppressing VEGFR-induced tube formation (IC50 33 nmol/L) as it does in inhibiting the proliferation of FGFR-dependent cell lines, including H1581, SNU16, and RT4 cells (IC50 50-150 nmol/L) in assays involving cells
In vitro, ODM-203 inhibits VEGFR-induced tube formation with an IC50 of 33 nmol/L. It inhibits proliferation in FGFR-dependent cell lines such as H1581, SNU16, and RT4 cells with IC50s of 50-150 nmol/L. Its activity is typically measured using kinase assays with purified enzymes and cell-based proliferation assays. |
| ln Vivo |
ODM-203 exhibits potent antitumor activity at comparable well-tolerated doses in both angiogenic and FGFR-dependent xenograft models in vivo.
In vivo, ODM-203 exhibits strong anti-tumor activity and induces anti-tumor immunity. It is orally bioavailable. Its efficacy in animal models of cancer is well-documented, with significant tumor growth inhibition. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for ODM-203 involve kinase activity assays using purified FGFR1-4 and VEGFR1-3 enzymes. The compound's inhibitory activity is measured by monitoring the phosphorylation of a substrate peptide or protein in the presence of ATP. IC50 values are determined from dose-response curves.
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| Cell Assay |
Following an eight-dose concentration series up to 3 μmol/L for 96 hours, the test compounds were applied to the cells after allowing them to attach for the entire night.
In vitro cellular assays for ODM-203 are conducted in FGFR-dependent cell lines (e.g., H1581, SNU16, RT4) and VEGFR-dependent endothelial cells. Cells are treated with the compound, and cell proliferation is measured using assays such as MTT or CellTiter-Glo. Tube formation assays using endothelial cells are performed to assess inhibition of angiogenesis. |
| Animal Protocol |
Subcutaneous Renca syngenic model
20 and 40 mg/kg Oral gavage In vivo animal studies for ODM-203 are conducted in mouse xenograft models using cancer cell lines sensitive to FGFR or VEGFR inhibition. Animals are administered the compound orally, and tumor growth inhibition is monitored. The compound's effects on angiogenesis and tumor immunity are assessed by immunohistochemistry and flow cytometry. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of ODM-203 indicate it has a molecular weight of 505.54 and a molecular formula of C26H21F2N5O2S. It is orally bioavailable. Its solubility and other PK parameters would be determined in preclinical studies. The compound is typically stored as a powder at appropriate conditions.
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| Toxicity/Toxicokinetics |
Toxicological information for ODM-203 is limited to preclinical studies. As a kinase inhibitor targeting angiogenesis and cell proliferation, it may have effects on wound healing, vascular function, and reproductive health. Comprehensive toxicology studies would be required for clinical development.
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| References | |
| Additional Infomation |
ODM-203, a VEGFR/FGFR inhibitor, is an orally administered inhibitor of human vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) with potential anti-angiogenic and anti-tumor activities. ODM-203 simultaneously inhibits both VEGFR and FGFR, thereby suppressing VEGFR and FGFR-mediated signaling pathways. This inhibits angiogenesis and cell proliferation in tumor cells overexpressing VEGFR and/or FGFR. Both VEGFR and FGFR belong to the receptor tyrosine kinase superfamily and are highly expressed in various tumor cell types.
ODM-203 is a potent inhibitor of FGFR and VEGFR families with strong anti-tumor activity. It is orally bioavailable. It is being investigated for the treatment of cancer. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use. |
| Molecular Formula |
C26H21F2N5O2S
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|---|---|
| Molecular Weight |
505.53905081749
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| Exact Mass |
505.138
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| Elemental Analysis |
C, 61.77; H, 4.19; F, 7.52; N, 13.85; O, 6.33; S, 6.34
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| CAS # |
1430723-35-5
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| Related CAS # |
1430723-35-5
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| PubChem CID |
71554322
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| Appearance |
White to yellow solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
886
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZJFCBQXPTQSTCZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H21F2N5O2S/c1-32-14-18(13-30-32)16-2-7-26-25(10-16)29-15-33(26)21-9-17(23-6-3-19(27)11-24(23)28)8-20(12-21)31-36(34,35)22-4-5-22/h2-3,6-15,22,31H,4-5H2,1H3
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| Chemical Name |
N-[3-(2,4-difluorophenyl)-5-[5-(1-methylpyrazol-4-yl)benzimidazol-1-yl]phenyl]cyclopropanesulfonamide
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| Synonyms |
ODM-203; ODM203; ODM 203
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 66.7~100 mg/mL (131.9~197.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1978 mL | 0.9890 mL | 1.9781 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03240445 | Completed | Drug: ODM-203 (Period 1) Drug: ODM-203 (Period 2) |
Healthy | Orion Corporation, Orion Pharma | August 24, 2017 | Phase 1 |
| NCT02264418 | Completed | Drug: ODM 203 | Solid Tumours | Orion Corporation, Orion Pharma | September 18, 2014 | Phase 1 |
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