Art. -Nr.: HY-19928

Vactosertib

(Synonyms: EW-7197; TEW-7197)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

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.

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Reinheit: 99.53%
CAS. Nr.: 1352608-82-2
Formel: C₂₂H₁₈FN₇
Molecular Weight:399.42

Speicherung:

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

Vactosertib Chemical Structure

CAS. Nr.: 1352608-82-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ALK5

12.9 nM (IC₅₀)

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

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]
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]
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]
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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1352608-82-2
Appearance Solid
Molecular Weight 399.42
Formel C₂₂H₁₈FN₇
Color Off-white to yellow
SMILES

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

EW-7197; TEW-7197
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (13)

All Flow CytometryWBRT-PCRCell Migration/Invasion Assay

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Journal Impact Factor

Nat Commun

The TGFβ type I receptor kinase inhibitor vactosertib in combination with pomalidomide in relapsed/refractory multiple myeloma: a phase 1b trial. [Abstract]

2024 Aug 27;15(1):7388. PMID: 39191755
Cell Discov

Single-cell transcriptome reveals cellular hierarchies and guides p-EMT-targeted trial in skull base chordoma. [Abstract]

2022 Sep 20;8(1):94. PMID: 36127333

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.
J Exp Med

Tumor-associated neutrophils attenuate the immunosensitivity of hepatocellular carcinoma. [Abstract]

2025 Jan 6;222(1):e20241442. PMID: 39636298
Lab Chip

DCMiC: a double-cylinder micro-chamber platform for high-throughput drug screening and modeling of microenvironmental resistance in Ewing sarcoma. [Abstract]

2025 Dec 9:10.1039/d5lc00856e. PMID: 41362255
Cancers

CXCR4 Inhibition Enhances Efficacy of FLT3 Inhibitors in FLT3-Mutated AML Augmented by Suppressed TGF-b Signaling. [Abstract]

2020 Jun 30;12(7):1737. PMID: 32629802

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.
Cancer Sci

TGF-β Inhibitor Potentiates Osimertinib-Induced Anti-Tumor Immunity in Egfr-Mutant Lung Cancer. [Abstract]

2026 Feb 27. PMID: 41757675
J Cell Mol Med

Pharmacological Targeting of DHHC9-Mediated STRN4 Palmitoylation to Suppress YAP-Driven Cancer Metastasis. [Abstract]

2025 Sep;29(17):e70815. PMID: 40903842
Exp Cell Res

Vactosertib reverses ABCG2-mediated multidrug resistance through dual inhibition of drug efflux and transporter expression. [Abstract]

2026 Aug 1;461(1):115098. PMID: 42264120
Dev Growth Differ

Transforming growth factor-β-mediated regulation of atoh1-expressing neural progenitors is involved in the generation of cerebellar granule cells in larval and adult zebrafish. [Abstract]

2025 Apr;67(3):149-164. PMID: 40012512
bioRxiv

2026 Jun 26.
bioRxiv

2026 May 19.
Patent

US20240197729A1.
Res Sq

Vactosertib, a novel TGF-β1 type I receptor kinase inhibitor, improves T-cell fitness: a single-arm, phase 1b trial in relapsed/refractory multiple myeloma. [Abstract]

2023 Jul 17:rs.3.rs-3112163. PMID: 37503043

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

13 Cited Publications

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Vactosertib

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Vactosertib

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vactosertib Related Classifications

HY-19928 Related Classifications