Vactosertib (Synonyms: EW-7197; TEW-7197)

Name: Vactosertib
Brand: MedChemExpress
SKU: HY-19928
Rating: 5.0 (10 reviews)

Cat. No.: HY-19928 Purity: 99.53%: Data Sheet
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Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC₅₀ of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC₅₀ of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.

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

CAS No. : 1352608-82-2

Size	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Vactosertib:

Vactosertib Hydrochloride In-stock

10 Publications Citing Use of MCE Vactosertib

Flow Cytometry

RT-PCR

Cell Migration/Invasion Assay

: Vactosertib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]; Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI protein levels in the UM‑Chor1 cell line.

: Vactosertib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]; Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI mRNA levels in the UM‑Chor1 cell line.

: Vactosertib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94. [Abstract]; Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h attenuated the invasiveness of UM‑Chor1 cells.

: Vactosertib purchased from MedChemExpress. Usage Cited in: Cancers. 2020 Jun 30;12(7):1737. [Abstract]; Vactosertib (1 nM, 72 h) in co-culture of MOLM-14 cells with TGF-β knockdown hMSC enhanced apoptosis induced by quizartinib (1 μM, 72 h), and even more so by the combined treatment.

: Vactosertib purchased from MedChemExpress. Usage Cited in: Cancers. 2020 Jun 30;12(7):1737. [Abstract]; Vactosertib (1 nM， 72 h) in co-culture of MOLM-14 cells with TGF-β knock-down hMSC showed effective blockade of CXCR4.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ALK5

12.9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.0121 μM Compound: 12b, EW-7197	Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	[PMID: 24786585]
HEK293	IC₅₀	31.04 μM Compound: 12b, EW-7197	Inhibition of human ERG channel expressed in HEK293 cells after 3 to 5.7 mins by whole-cell patch clamp technique Inhibition of human ERG channel expressed in HEK293 cells after 3 to 5.7 mins by whole-cell patch clamp technique	[PMID: 24786585]
HaCaT	IC₅₀	0.0165 μM Compound: 12b, EW-7197	Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	[PMID: 24786585]
Sf9	IC₅₀	0.007 μM Compound: 12b, EW-7197	Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay	[PMID: 24786585]
Sf9	IC₅₀	0.01 μM Compound: 4; EW-7197	Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay	[PMID: 31299584]
Sf9	IC₅₀	0.014 μM Compound: 4; EW-7197	Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method	[PMID: 31303386]
Sf9	IC₅₀	9.67 nM Compound: 5; EW-7197	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay	[PMID: 26483198]

In Vitro

Vactosertib (10-1000 nM; 30 minutes; 4T1 cells) treatment blocks the TGFβ-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner in 4T1 cells^[1].
? Vactosertib suppresses the TGFβ-induced nuclear translocation of Smad2/3 in 4T1 cells and MCF10A cells. The IC₅₀ value of Vactosertib on pSmad3 in 4T1 cells is 10-30 nM^[1].
? Vactosertib abrogates TGFb1-induced tumor cell migration and invasion^[1].
? TGFβ1 downregulated the mRNA level of CDH1 and upregulated the mRNA levels of FN1, HMGA2 (high-mobility group AT-hook 2), SNAI1, and SNAI2 (Snail family zinc finger 1 and 2, respectively). Moreover, Vactosertib abolishes the TGFβ1-induced effects on genes related to epithelial-to-mesenchymal transition (EMT)^[1].

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

Western Blot Analysis^[1]

Cell Line:	4T1 cells
Concentration:	10 nM, 30 µM, 50 nM, 100 µM, 300 nM, 500 nM, 1000 nM
Incubation Time:	30 minutes
Result:	Blocked the TGFb-induced phosphorylation of Smad2 or Smad3 in a dose-dependent manner.

In Vivo

Vactosertib (40 mg/kg; intraperitoneal injection; every other day; for 10 weeks; MMTV/c-Neu female mice) treatment inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice^[1].
? Vactosertib also inhibits the epithelial-to-mesenchymal transition (EMT) in both TGFβ-treated breast cancer cells and 4T1 orthotopic-grafted mice. Furthermore, Vactosertib enhances cytotoxic T lymphocyte activity in 4T1 orthotopic-grafted mice and increased the survival time of 4T1-Luc and 4T1 breast tumor-bearing mice^[1].

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

Animal Model:	Mammary tumor virus (MMTV)/c-Neu female mice (32-week-old)^[1]
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; every other day; for 10 weeks
Result:	Inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice.

Clinical Trial

Molecular Weight

399.42

Formula

C₂₂H₁₈FN₇

CAS No.

1352608-82-2

Appearance

Solid

Color

Off-white to yellow

SMILES

CC1=CC=CC(C2=C(C3=CN4C(C=C3)=NC=N4)NC(CNC5=CC=CC=C5F)=N2)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (250.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (250.36 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5036 mL	12.5182 mL	25.0363 mL
5 mM	0.5007 mL	2.5036 mL	5.0073 mL
10 mM	0.2504 mL	1.2518 mL	2.5036 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.26 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.53%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (253 KB) HNMR (263 KB) RP-HPLC (246 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Son JY et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis, 2014 Jul, 13(7):1704-16. [Content Brief]

[2]. Naka K, et al. Novel oral transforming growth factor-β signaling inhibitor EW-7197 eradicates CML-initiating cells. Cancer Sci. 2016 Feb;107(2):140-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	2.5036 mL	12.5182 mL	25.0363 mL	62.5908 mL
	5 mM	0.5007 mL	2.5036 mL	5.0073 mL	12.5182 mL
	10 mM	0.2504 mL	1.2518 mL	2.5036 mL	6.2591 mL
	15 mM	0.1669 mL	0.8345 mL	1.6691 mL	4.1727 mL
	20 mM	0.1252 mL	0.6259 mL	1.2518 mL	3.1295 mL
	25 mM	0.1001 mL	0.5007 mL	1.0015 mL	2.5036 mL
	30 mM	0.0835 mL	0.4173 mL	0.8345 mL	2.0864 mL
	40 mM	0.0626 mL	0.3130 mL	0.6259 mL	1.5648 mL
	50 mM	0.0501 mL	0.2504 mL	0.5007 mL	1.2518 mL
	60 mM	0.0417 mL	0.2086 mL	0.4173 mL	1.0432 mL
	80 mM	0.0313 mL	0.1565 mL	0.3130 mL	0.7824 mL
	100 mM	0.0250 mL	0.1252 mL	0.2504 mL	0.6259 mL

Vactosertib 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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Vactosertib (Synonyms: EW-7197; TEW-7197)

Customer Review

Other Forms of Vactosertib:

Vactosertib Related Antibodies

10 Publications Citing Use of MCE Vactosertib

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TGF-β Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Vactosertib Related Antibodies

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Complete Stock Solution Preparation Table

Vactosertib Related Classifications

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