| Identification | Back Directory | [Name]
ODM203 | [CAS]
1430723-35-5 | [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]- | [Molecular Formula]
C26H21F2N5O2S | [MDL Number]
MFCD32062783 | [MOL File]
1430723-35-5.mol | [Molecular Weight]
505.54 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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.
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| 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.
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| 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.
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| [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) | [storage]
Store at -20°C | [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 |
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