ODM-203
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.
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- Pureza: 99.62%
- No. CAS: 1430723-35-5
- Fòrmula: C26H21F2N5O2S
- Peso molecular:505.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
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.
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Cell Line:H1581 (ATCC-CRL-5878), SNU16 (ATCC-CRL-5974) and RT4 (HTB2) cells
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Concentration:Eight-dose concentration series up to 3 μM
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Incubation Time:96 h
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Result:Suppressed cell proliferation in a dose-dependent manner in H1581 (IC50=104 nM), SNU16 (IC50=132 nM) and RT4 cells (IC50=192 nM).
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Cell Line:HUVECs and human umbilical vein endothelial cells (co-culture)
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Concentration:Eight-dose concentration series up to 3 μM
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Incubation Time:10 days (media and test agents were replaced every 2-3 days)
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Result:Inhibited endothelial tubule formation in a dose-dependent manner at non-toxic concentrations with an IC50 value of 33 nM.
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Cell Line:HUVEC cells
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:1 h
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Result:Suppressed both FGFR and VEGFR signaling.
In Vivo
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.
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Animal Model:Athymic Nude-Foxn1nu female mice (9-week-old; subcutaneous xenograft models)[1].
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Dosage:20, 40 mg/kg
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Administration:Oral administration; single daily for 21 days.
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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.
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Animal Model:Male balb/c mice (8-week-old; orthotopic renca syngenic model)[1].
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Dosage:7, 20, 40 mg/kg
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Administration:Oral administration; single daily for 21 days.
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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.
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Animal Model:Male balb/c male mice (5 to 7-week-old; renca subcutaneous tumor model)[1].
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Dosage:20, 40 mg/kg
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Administration:Oral administration; single daily for 5 days.
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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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1430723-35-5
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Appearance Solid
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Peso molecular 505.54
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Fòrmula C26H21F2N5O2S
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Color White to yellow
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SMILES
CN(N=C1)C=C1C2=CC=C3C(N=CN3C4=CC(C5=CC=C(F)C=C5F)=CC(NS(C6CC6)(=O)=O)=C4)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| 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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