Vactosertib
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MedKoo CAT#: 558278

CAS#: 1352608-82-2

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 mice.


Chemical Structure

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Vactosertib
CAS# 1352608-82-2

Theoretical Analysis

MedKoo Cat#: 558278
Name: Vactosertib
CAS#: 1352608-82-2
Chemical Formula: C22H18FN7
Exact Mass: 399.16077
Molecular Weight: 399.42
Elemental Analysis: C, 66.15; H, 4.54; F, 4.76; N, 24.55

Size Price Shipping out time Quantity
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 850 Same day
500mg USD 1850 Same day
1g USD 3250 Same day
2g USD 5850 Same day
Inquire bulk and customized quantity

Pricing updated 2021-02-28. Prices are subject to change without notice.

Vactosertib, purity > 98%, is in stock. The same day shipping after order is received.

Synonym: TEW7197; TEW 7197; TEW-7197; Vactosertib

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

InChi Key: FJCDSQATIJKQKA-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H18FN7/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)

SMILES Code: FC1=CC=CC=C1NCC2=NC(C3=CN4C(C=C3)=NC=N4)=C(C5=NC(C)=CC=C5)N2

Appearance:
white solid powder

Purity:
>99% (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, not in water

Shelf Life:
>2 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

Preparing Stock Solutions

The following data is based on the product molecular weight 399.42 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Son JY, Park SY, Kim SJ, Lee SJ, Park SA, Kim MJ, Kim SW, Kim DK, Nam JS, Sheen YY. EW-7197, A Novel ALK-5 Kinase Inhibitor, Potently Inhibits Breast to Lung Metastasis. Mol Cancer Ther. 2014 May 9. [Epub ahead of print] PubMed PMID: 24817629.

2: 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.

3: Sheen YY, Kim MJ, Park SA, Park SY, Nam JS. Targeting the Transforming Growth Factor-β Signaling in Cancer Therapy. Biomol Ther (Seoul). 2013 Sep 30;21(5):323-331. Review. PubMed PMID: 24244818; PubMed Central PMCID: PMC3825194.

4: Yoon JH, Jung SM, Park SH, Kato M, Yamashita T, Lee IK, Sudo K, Nakae S, Han JS, Kim OH, Oh BC, Sumida T, Kuroda M, Ju JH, Jung KC, Park SH, Kim DK, Mamura M. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4, thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol Med. 2013 Nov;5(11):1720-39. doi: 10.1002/emmm.201302524. Epub 2013 Oct 11. Erratum in: EMBO Mol Med. 2014 May;6(5):703. PubMed PMID: 24127404; PubMed Central PMCID: PMC3840488.



Additional Information