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5mg |
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25mg |
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50mg |
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100mg |
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ODM-203 is a potent and orally bioavailable inhibitor of FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively. ODM-203 has potent antiangiogenic and antitumorous properties. Both VEGFRs and FGFRs are inhibited by the VEGFR/FGFR inhibitor ODM-203, which may lead to the inhibition of VEGFR- and FGFR-mediated signaling. When tumor cells overexpress VEGFR and/or FGFR, this results in the inhibition of angiogenesis and cell proliferation. Both FGFRs and VEGFRs are members of the receptor tyrosine kinase superfamily and are expressed at elevated levels in different types of tumor cells.
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)
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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
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ln Vivo |
ODM-203 exhibits potent antitumor activity at comparable well-tolerated doses in both angiogenic and FGFR-dependent xenograft models in vivo.
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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.
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Animal Protocol |
Subcutaneous Renca syngenic model
20 and 40 mg/kg Oral gavage |
References |
Molecular Formula |
C26H21F2N5O2S
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Molecular Weight |
505.54
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Exact Mass |
505.1384
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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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Appearance |
Solid powder
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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
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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 |
Chemical structures of ODM-203 and the reference compounds described in this article. Mol Cancer Ther . 2019 Jan;18(1):28-38. td> |
ODM-203 is equally potent at inhibiting FGFR and VEGFR phosphorylation in cells. Mol Cancer Ther . 2019 Jan;18(1):28-38. td> |
ODM-203 suppresses in vivo tumor growth and FGFR signaling in FGFR-dependent tumor models. Mol Cancer Ther . 2019 Jan;18(1):28-38. td> |
ODM-203 has strong in vivo antitumor activity in an angiogenic model. Mol Cancer Ther . 2019 Jan;18(1):28-38. td> |