Vactosertib HCl | CAS# 1352610-25-3 | TGF-β Type 1 Receptor Kinase Inhibitor

MedKoo Cat#: 565040 | Name: Vactosertib HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Chemical Structure

Vactosertib HCl

CAS#1352610-25-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 565040

Name: Vactosertib HCl

CAS#: 1352610-25-3 (HCl)

Chemical Formula: C22H19ClFN7

Exact Mass: 435.1374

Molecular Weight: 435.89

Elemental Analysis: C, 60.62; H, 4.39; Cl, 8.13; F, 4.36; N, 22.49

Price and Availability

Size	Price	Availability
5mg	USD 310.00	2 weeks
10mg	USD 510.00	2 weeks
25mg	USD 940.00	2 weeks

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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

Product Data

Product Data

Instruction

View handling instruction

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	mg/mL	mM
Solubility
	DMSO	50.0	114.71
	Water	50.0	114.71

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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:

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.