EW-7195

小分子

EW-7195

E647270-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC 50 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MMTV/c-Neu mice 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. Animal Model: Balb/c xenograft model (10-weeks-old female Balb/c mice bearing 4T1 cells) 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. Form:Solid IC50& Target:ALK5 4.83 nM (IC 50 ) p38α 1.5 μM (IC 50 )

EW-7195 是一种强效、选择性 ALK5（TGFβR1）抑制剂，其 IC 50 为 4.83 nM。与 p38α 相比，EW-7195 对 ALK5 的选择性大于 300 倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮细胞向间质转化（EMT）和乳腺癌的发生。

1352609-28-9

C23H18N8

406.44 g/mol

N#CC1=CC=CC(NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2)=C1

DMSO : 50 mg/mL (123.02 mM; Need ultrasonic)