ODM203
ODM203 Basic information
- Product Name:
- ODM203
- Synonyms:
-
- ODM203
- N-[2',4'-Difluoro-5-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl][1,1'-biphenyl]-3-yl]cyclopropanesulfonamide
- Cyclopropanesulfonamide, N-[2',4'-difluoro-5-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl][1,1'-biphenyl]-3-yl]-
- N-(2',4'-Difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-3-yl)cyclopropanesulfonamide
- anti-tumor immunity,ODM-203,FGFR,HUVEC,H1581,Inhibitor,cancer,Vascular endothelial growth factor receptor,SNU16,ODM203,ODM 203,RT4,Fibroblast growth factor receptor,VEGFR,inhibit
- ODM-203, 10 mM in DMSO
- ODM-203 ，S8882
- CAS:
- 1430723-35-5
- MF:
- C26H21F2N5O2S
- MW:
- 505.54
- Mol File:
- 1430723-35-5.mol
ODM203 Chemical Properties
- Boiling point:
- 732.4±70.0 °C(Predicted)
- Density
- 1.48±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 66.67 mg/mL (131.88 mM; Need ultrasonic)
- form
- A crystalline solid
- pka
- 7.88±0.20(Predicted)
- color
- White to yellow
ODM203 Usage And Synthesis
Uses
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].
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].
| 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. |
IC 50
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)
References
[1] Holmstr?m 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. DOI:10.1158/1535-7163.MCT-18-0204
ODM203Supplier
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