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  3. (Rac)-NSC305787 hydrochloride

NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.

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

(Rac)-NSC305787 hydrochloride Chemical Structure

(Rac)-NSC305787 hydrochloride Chemical Structure

CAS No. : 53868-26-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 462 In-stock
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 540 In-stock
50 mg USD 1490 In-stock
100 mg USD 1990 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of (Rac)-NSC305787 hydrochloride:

Top Publications Citing Use of Products

    (Rac)-NSC305787 hydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2020 Aug 1;254:117681.  [Abstract]

    NSC305787 considerably inhibits the expression of p-ezrin, RhoA, RohC and ROCK1 without altering cellular ezrin levels at 2.5 μM and 5 μM.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.

    IC50 & Target

    Kd: 5.85 μM (ezrin)[1]
    IC50: 8.3 μM (ezrin)[1]

    In Vitro

    NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC50s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a Kd value of 172.4 μM, and inhibits ezrin T567 phosphorylation primarily via its binding to ezrin and not through inhibition of PKCΙ kinase activity. NSC305787 (1, 10 μM) shows inhibitory activity against ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells. Moreover, NSC305787 (10 μM) reduces cell motility phenotypes in zebrafish and blocks OS metastatic growth in lung organ culture[1].

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

    In Vivo

    NSC305787 (0.240 mg/kg/day, i.p.) suppresses ezrin-dependent osteosarcoma metastatic growth in mouse lung[1]. NSC305787 (240 μg/kg, i.p.) dramatically inhibits pulmonary metastasis in a transgenic mouse model of osteosarcoma (Osx-Cre+p53fl/flpRBfl/fl) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model[2].

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

    Molecular Weight

    481.89

    Formula

    C25H31Cl3N2O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC(C1CCCCN1)C2=CC(C3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3)=NC(C(Cl)=C6)=C2C=C6Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 8 mg/mL (16.60 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0752 mL 10.3758 mL 20.7516 mL
    5 mM 0.4150 mL 2.0752 mL 4.1503 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 (sealed storage, 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 1.25 mg/mL (2.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    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:
    %
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    %
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    %
    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 (sealed storage, 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: 99.07%

    References
    Cell Assay
    [1]

    Human umbilical vein endothelial cells (HUVECs; 2.5 × 104/well) are seeded in a 96-well plate in endothelial growth media-2. Following formation of a confluent HUVEC monolayer (∼32 h), endothelial growth media-2 is aspirated and a layer of osteosarcoma (OS) cells (1.0 × 104 cells/well) is added to Dulbecco’s modified Eagle medium containing NSC305787. This specific time point is accepted as 0 h of treatment, and invasion is monitored during the subsequent 5 h by measuring changes in resistance at the cell-electrode interphase. The cell index is calculated according to the following formula: cell index = (Rt – R0)/F, where Rt is resistance at time point t, R0 is background resistance (measured with media alone, no cells) and F is frequency at which the measurement is taken (10 kHz)[1].

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

    Animal Administration
    [2]

    Mice[2]
    The Osx-Cre+p53fl/flpRBfl/fl transgenic mouse model of osteosarcoma is used in the assay. Mice are treated with 240 μg/kg/day NSC305787, 226 μg/kg/day NSC668394, or vehicle (DMSO, 1%) once daily, five times a week by i.p. injection in a volume of 100 μL. At the end of the study, lung and tumor samples are isolated upon necropsy. Half of each sample is flash frozen immediately in liquid nitrogen, and the other half is fixed in 10% formalin for 18-24 h, transferred to 70% ethanol, and stored at room temperature[2].

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

    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 (sealed storage, 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 2.0752 mL 10.3758 mL 20.7516 mL 51.8791 mL
    5 mM 0.4150 mL 2.0752 mL 4.1503 mL 10.3758 mL
    10 mM 0.2075 mL 1.0376 mL 2.0752 mL 5.1879 mL
    15 mM 0.1383 mL 0.6917 mL 1.3834 mL 3.4586 mL
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    • 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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    Product Name:
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