WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H565040
CAS#: 1352610-25-3 (HCl)
Description: Vactosertib, also known as TEW-7197 is a potent ALK5 inhibitor. TEW-7197 showed potent in vivo anti-metastatic activity, indicating its potential for use as an anti-cancer therapy. EW-7197 inhibits TGF-β/Smad signaling. EW-7197 abrogates TGF-β1-induced tumor cell migration and invasion. EW-7197 inhibits breast cancer metastasis to the lung.EW-7197 prolongs the life span of BALB/c 4T1 mice via inhibition of EMT. EW-7197 inhibits metastasis and enhances the activity of cytotoxic T lymphocytes (CTLs) in 4T1 orthotopic grafted mic
Hodoodo Cat#: H565040
Name: Vactosertib HCl
CAS#: 1352610-25-3 (HCl)
Chemical Formula: C22H19ClFN7
Exact Mass: 435.14
Molecular Weight: 435.890
Elemental Analysis: C, 60.62; H, 4.39; Cl, 8.13; F, 4.36; N, 22.49
Related CAS #: 1352608-82-2 (free base) 1352610-25-3 (HCl)
Synonym: EW-7197 Hydrochloride; EW7197 HCl; EW 7197 HCl; EW-7197 HCl; Vactosertib HCl; Vactosertib hydrochloride
IUPAC/Chemical Name: N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline hydrochloride
InChi Key: UDRJLVATGDHMJM-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H18FN7.ClH/c1-14-5-4-8-18(27-14)22-21(15-9-10-20-25-13-26-30(20)12-15)28-19(29-22)11-24-17-7-3-2-6-16(17)23;/h2-10,12-13,24H,11H2,1H3,(H,28,29);1H
SMILES Code: FC1=CC=CC=C1NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2.Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. |
| In vitro activity: | When A549-CUG2 and BEAS-CUG2 cells were treated with EW-7197 at different concentrations, E-cadherin protein levels recovered in a dose-dependent manner in A549-CUG2 cells but simply recovered in BEAS-CUG2 cells (Figure 6A). N-cadherin and vimentin protein levels gradually decreased in a dose-dependent manner in A549-CUG2 and BEAS-CUG2 cells (Figure 6A). In contrast to TGF-β treatment, EW-7197 treatment gradually reduced CUG2 protein levels in a dose-dependent manner (Figure 6A). Reference: Oncotarget. 2017 Jan 17; 8(3): 5092–5110. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5354895/ |
| In vivo activity: | EW-7197 treatment ameliorates acquired lymphedema in a mouse tail model by increasing lymphangiogenesis and interstitial flow of the lymphatics by inhibition of the fibrosis. The differences in maximal tail thicknesses between the control and treatment groups were statistically significant from 2 to 4 weeks after surgery. The treatment group showed a greater number of lymphatic vessels at the surgery site than the control group. The treatment group also showed more FITC coverage area at the surgery site. Reference: Lymphat Res Biol. 2020 Oct;18(5):433-438. https://pubmed.ncbi.nlm.nih.gov/32105567/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.0 | 114.71 | |
| Water | 50.0 | 114.71 |
The following data is based on the product molecular weight 435.89 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Kaowinn S, Kim J, Lee J, Shin DH, Kang CD, Kim DK, Lee S, Kang MK, Koh SS, Kim SJ, Chung YH. Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-β signaling. Oncotarget. 2017 Jan 17;8(3):5092-5110. doi: 10.18632/oncotarget.13867. PMID: 27974707; PMCID: PMC5354895. 2. Naka K, Ishihara K, Jomen Y, Jin CH, Kim DH, Gu YK, Jeong ES, Li S, Krause DS, Kim DW, Bae E, Takihara Y, Hirao A, Oshima H, Oshima M, Ooshima A, Sheen YY, Kim SJ, Kim DK. Novel oral transforming growth factor-β signaling inhibitor EW-7197 eradicates CML-initiating cells. Cancer Sci. 2016 Feb;107(2):140-8. doi: 10.1111/cas.12849. Epub 2016 Jan 26. PMID: 26583567; PMCID: PMC4768399. 3. Yoon SH, Kim KY, Wang Z, Park JH, Bae SM, Kim SY, Song HY, Jeon JY. EW-7197, a Transforming Growth Factor-Beta Type I Receptor Kinase Inhibitor, Ameliorates Acquired Lymphedema in a Mouse Tail Model. Lymphat Res Biol. 2020 Oct;18(5):433-438. doi: 10.1089/lrb.2018.0070. Epub 2020 Feb 27. PMID: 32105567. 4. Soleimani A, Asgharzadeh F, Rahmani F, Avan A, Mehraban S, Fakhraei M, Arjmand MH, Binabaj MM, Parizadeh MR, Ferns GA, Ryzhikov M, Afshari AR, Naghinezhad J, Sayyed-Hosseinian SH, Khazaei M, Hassanian SM. Novel oral transforming growth factor-β signaling inhibitor potently inhibits postsurgical adhesion band formation. J Cell Physiol. 2020 Feb;235(2):1349-1357. doi: 10.1002/jcp.29053. Epub 2019 Jul 17. PMID: 31313829. |
| In vitro protocol: | 1. Kaowinn S, Kim J, Lee J, Shin DH, Kang CD, Kim DK, Lee S, Kang MK, Koh SS, Kim SJ, Chung YH. Cancer upregulated gene 2 induces epithelial-mesenchymal transition of human lung cancer cells via TGF-β signaling. Oncotarget. 2017 Jan 17;8(3):5092-5110. doi: 10.18632/oncotarget.13867. PMID: 27974707; PMCID: PMC5354895. 2. Naka K, Ishihara K, Jomen Y, Jin CH, Kim DH, Gu YK, Jeong ES, Li S, Krause DS, Kim DW, Bae E, Takihara Y, Hirao A, Oshima H, Oshima M, Ooshima A, Sheen YY, Kim SJ, Kim DK. Novel oral transforming growth factor-β signaling inhibitor EW-7197 eradicates CML-initiating cells. Cancer Sci. 2016 Feb;107(2):140-8. doi: 10.1111/cas.12849. Epub 2016 Jan 26. PMID: 26583567; PMCID: PMC4768399. |
| In vivo protocol: | 1. Yoon SH, Kim KY, Wang Z, Park JH, Bae SM, Kim SY, Song HY, Jeon JY. EW-7197, a Transforming Growth Factor-Beta Type I Receptor Kinase Inhibitor, Ameliorates Acquired Lymphedema in a Mouse Tail Model. Lymphat Res Biol. 2020 Oct;18(5):433-438. doi: 10.1089/lrb.2018.0070. Epub 2020 Feb 27. PMID: 32105567. 2. Soleimani A, Asgharzadeh F, Rahmani F, Avan A, Mehraban S, Fakhraei M, Arjmand MH, Binabaj MM, Parizadeh MR, Ferns GA, Ryzhikov M, Afshari AR, Naghinezhad J, Sayyed-Hosseinian SH, Khazaei M, Hassanian SM. Novel oral transforming growth factor-β signaling inhibitor potently inhibits postsurgical adhesion band formation. J Cell Physiol. 2020 Feb;235(2):1349-1357. doi: 10.1002/jcp.29053. Epub 2019 Jul 17. PMID: 31313829. |
1: Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Lee HJ, Park SJ, Park HJ, Lee K, Sheen YY, Kim DK. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2 -yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem. 2014 May 22;57(10):4213-38. doi: 10.1021/jm500115w. Epub 2014 May 13. PubMed PMID: 24786585.
