1. TGF-beta/Smad MAPK/ERK Pathway
  2. TGF-β Receptor p38 MAPK
  3. EW-7195

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.

For research use only. We do not sell to patients.

EW-7195 Chemical Structure

EW-7195 Chemical Structure

CAS No. : 1352609-28-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 440 In-stock
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3500 In-stock
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Based on 1 publication(s) in Google Scholar

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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[1].

IC50 & Target[1]

ALK5

4.83 nM (IC50)

p38α

1.5 μM (IC50)

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[1].
EW-7195 (0.5-1 µM; 1.5 hours) efficiently inhibits TGF-β1-induced Smad2 phosphorylation[1].

MedChemExpress (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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.
Molecular Weight

406.44

Formula

C23H18N8

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (123.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4604 mL 12.3019 mL 24.6039 mL
5 mM 0.4921 mL 2.4604 mL 4.9208 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4604 mL 12.3019 mL 24.6039 mL 61.5097 mL
5 mM 0.4921 mL 2.4604 mL 4.9208 mL 12.3019 mL
10 mM 0.2460 mL 1.2302 mL 2.4604 mL 6.1510 mL
15 mM 0.1640 mL 0.8201 mL 1.6403 mL 4.1006 mL
20 mM 0.1230 mL 0.6151 mL 1.2302 mL 3.0755 mL
25 mM 0.0984 mL 0.4921 mL 0.9842 mL 2.4604 mL
30 mM 0.0820 mL 0.4101 mL 0.8201 mL 2.0503 mL
40 mM 0.0615 mL 0.3075 mL 0.6151 mL 1.5377 mL
50 mM 0.0492 mL 0.2460 mL 0.4921 mL 1.2302 mL
60 mM 0.0410 mL 0.2050 mL 0.4101 mL 1.0252 mL
80 mM 0.0308 mL 0.1538 mL 0.3075 mL 0.7689 mL
100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6151 mL
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EW-7195 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
EW-7195
Cat. No.:
HY-18766
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