| Identification | Back Directory | [Name]
EW-7195 | [CAS]
1352609-28-9 | [Synonyms]
EW-7195
Benzonitrile, 3-[[[5-(6-methyl-2-pyridinyl)-4-[1,2,4]triazolo[1,5-a]pyridin-6-yl-1H-imidazol-2-yl]methyl]amino]- | [Molecular Formula]
C23H18N8 | [MOL File]
1352609-28-9.mol | [Molecular Weight]
406.44 |
| Chemical Properties | Back Directory | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (123.02 mM; Need ultrasonic) | [form ]
Solid | [pka]
8.52±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung[1]. | [in vivo]
EW7195 (40 mg/kg; i.p.; three times a week for 3/2.5 weeks) inhibits lung metastasis development in both 4T1 orthotopic xenograft and MMTV/cNeu transgenic mice[1]. | Animal Model: | MMTV/c-Neu mice[1] | | Dosage: | 40 mg/kg | | Administration: | I.p.; three times a week for 3 weeks | | Result: | Inhibited the metastasis of breast cancer cells to the lung.
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| Animal Model: | Balb/c xenograft model (10-weeks-old female Balb/c mice bearing 4T1 cells)[1] | | Dosage: | 40 mg/kg | | Administration: | I.p.; three times a week for 2.5 weeks | | Result: | Suppressed a lung metastasis in the Balb/c Xenograft model.
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| [IC 50]
ALK5: 4.83 nM (IC50); p38α: 1.5 μM (IC50) | [References]
[1] Park CY, et al. EW-7195, a novel inhibitor of ALK5 kinase inhibits EMT and breast cancer metastasis to lung. Eur J Cancer. 2011;47(17):2642-2653. DOI:10.1016/j.ejca.2011.07.007 |
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