2. TGF-beta/Smad
  3. TGF-β Receptor
  4. Vactosertib Hydrochloride

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

Cat. No.: HY-19928A Purity: 99.22%
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Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.

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

CAS No. : 1352610-25-3

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Vactosertib Hydrochloride:

Vactosertib Hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Vactosertib Hydrochloride 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 Hydrochloride 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 Hydrochloride 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 Hydrochloride 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 Hydrochloride 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.

    View All TGF-β Receptor Isoform Specific Products:

    View All Isoforms
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect[1][2].

    IC50 & Target[1]

    ALK5

    12.9 nM (IC50)

    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.

    Vactosertib Hydrochloride Related Antibodies

    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.
    Molecular Weight

    435.88

    Formula

    C22H19ClFN7
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, stored under nitrogen, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (229.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2942 mL 11.4710 mL 22.9421 mL
    5 mM 0.4588 mL 2.2942 mL 4.5884 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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (5.74 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 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 (5.74 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 25 mg/mL (57.36 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1 M HCl

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

    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: 99.22%

    SDS (393 KB)

    COA (254 KB) HNMR (399 KB) RP-HPLC (268 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References

    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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2942 mL 11.4710 mL 22.9421 mL 57.3552 mL
    5 mM 0.4588 mL 2.2942 mL 4.5884 mL 11.4710 mL
    10 mM 0.2294 mL 1.1471 mL 2.2942 mL 5.7355 mL
    15 mM 0.1529 mL 0.7647 mL 1.5295 mL 3.8237 mL
    20 mM 0.1147 mL 0.5736 mL 1.1471 mL 2.8678 mL
    25 mM 0.0918 mL 0.4588 mL 0.9177 mL 2.2942 mL
    30 mM 0.0765 mL 0.3824 mL 0.7647 mL 1.9118 mL
    40 mM 0.0574 mL 0.2868 mL 0.5736 mL 1.4339 mL
    50 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1471 mL
    60 mM 0.0382 mL 0.1912 mL 0.3824 mL 0.9559 mL
    80 mM 0.0287 mL 0.1434 mL 0.2868 mL 0.7169 mL
    100 mM 0.0229 mL 0.1147 mL 0.2294 mL 0.5736 mL
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    Vactosertib Hydrochloride 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.

    Keywords:

    Vactosertib1352610-25-3EW-7197TEW-7197EW7197EW 7197TEW7197TEW 7197TGF-β ReceptorTransforming growth factor beta receptorsTGFβSmadp38αantimetastaticbreastcancercellmigrationinvasionsurvivalInhibitorinhibitorinhibit

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