EW-7195 free base · Synonyms: EW 7195 · EW7195

EW-7195 is a potent and selective ALK5 inhibitor.

For research use only. Not for human or veterinary use.

Target TGF-β Receptor p38 MAPK

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

EW-7195 structure

CAS No.: 1352609-28-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 mg	USD 420.00	BP-01875-10mg	In stock	Get quote
25 mg	USD 620.00	BP-01875-25mg	In stock	Get quote
50 mg	USD 920.00	BP-01875-50mg	In stock	Get quote
250 mg	USD 1,820.00	BP-01875-250mg	In stock	Get quote
1 g	Inquire	BP-01875-1g	Inquire	Inquire

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Description

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.

Biological activity

In Vitro EW7195 inhibits the EMT, motility, and invasiveness of breast cancer cells in vitro. EW-7195 efficiently blocks TGF-β1-induced phosphorylation of Smad2 followed by the nuclear translocation of Smad2/3. EW-7195 blocks TGF-β1-induced mesenchymal morphology. EW-7195 inhibits TGF-β-induced transcriptional activation. EW-7195 (0.5-1 μM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation. 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.

Identifiers

SMILES: N#CC1=CC=CC(NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2)=C1
InChIKey: KEADGKSQIBFYEE-UHFFFAOYSA-N

Specifications

MW (average): 406.4426
Formula: C₂₃H₁₈N₈
CAS No.: 1352609-28-9
Physical state: Solid
Color: off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 50 mg/mL

Documents

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.

Same target

Search TGF-β Receptor

Same research area

Search Cancer