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ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .

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

ISA-2011B Chemical Structure

ISA-2011B Chemical Structure

CAS No. : 1395347-24-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 319 In-stock
Solution
10 mM * 1 mL in DMSO USD 319 In-stock
Solid
1 mg USD 132 In-stock
5 mg USD 290 In-stock
10 mg USD 460 In-stock
50 mg USD 1400 In-stock
100 mg USD 2240 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 14 publication(s) in Google Scholar

ISA-2011B Related Antibodies

Top Publications Citing Use of Products

    ISA-2011B purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4117-4129.  [Abstract]

    Effect of ISA-2011B or its gene knockout on cancer cell proliferation. Colony formation assays are performed in SKBR3 cells treated with ISA-2011B (20 μM) or DMSO as a control.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .

    In Vitro

    The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is significantly reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively. ISA-2011B exhibits the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells[1]. ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR[2].

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

    ISA-2011B Related Antibodies
    In Vivo

    ISA-2011B significantly inhibits growth of tumor cells in xenograft mice, and is mediated by targeting PIP5K1α-associated PI3K/AKT and the downstream survival, proliferation, and invasion pathways[1]. Overexpression of AR-V7 increases PIP5K1α, promotes rapid growth of PCa in xenograft mice, whereas inhibition of PIP5K1α by its inhibitor ISA-2011B suppresses the growth and invasiveness of xenograft tumors overexpressing AR-V7. ISA-2011B disrupts protein stabilization of AR-V7 which is dependent on PIP5K1α, leading to suppression of invasive growth of AR-V7-high tumors in xenograft mice[2].

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

    423.85

    Formula

    C22H18ClN3O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1[C@H](C2=CNC3=C2C=C(Cl)C=C3)C4=C(C=C5C(OCO5)=C4)C[C@]16[H])CN(C)C6=O
    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 (235.93 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 2.3593 mL 11.7966 mL 23.5933 mL
    5 mM 0.4719 mL 2.3593 mL 4.7187 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)

    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 (5.90 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 (5.90 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:  0.5% CMC-Na/saline water

      Solubility: 4 mg/mL (9.44 mM); Suspended solution; Need ultrasonic

    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).
    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: 99.97%

    COA (261 KB) LCMS (99 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cells are grown in phenol red-free RPMI-1640 medium 24 hours and then are treated with drugs alone or in combination for 24 hours or 48 hours. MDV3100 at 5 μM or ISA-2011B at 20 μM or 50 μM final concentrations or solvent DMSO 1% is used. For treatment of 22Rv1 cells with MG132, a proteasome inhibitor, cells are treated with MG132 at 1 μM. For combination treatment of MG132 and ISA-2011B, cells are pre-treated with MG132 for 30 min at 1 μM prior to treatment of ISA-2011B[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: BALB/c nude mice aged 8 to 12 wk are used in the experiments. Tumor cells are implanted into the mice. Tumor xenografts are treated with vehicle (control), RP-56976 (10 mg/kg), ISA-2011B (40 mg/kg), and RP-56976 (10 mg/kg) in combination with ISA-2011B (40 mg/kg) every second day[1].

    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, 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 1 mM 2.3593 mL 11.7966 mL 23.5933 mL 58.9831 mL
    5 mM 0.4719 mL 2.3593 mL 4.7187 mL 11.7966 mL
    10 mM 0.2359 mL 1.1797 mL 2.3593 mL 5.8983 mL
    15 mM 0.1573 mL 0.7864 mL 1.5729 mL 3.9322 mL
    20 mM 0.1180 mL 0.5898 mL 1.1797 mL 2.9492 mL
    25 mM 0.0944 mL 0.4719 mL 0.9437 mL 2.3593 mL
    30 mM 0.0786 mL 0.3932 mL 0.7864 mL 1.9661 mL
    40 mM 0.0590 mL 0.2949 mL 0.5898 mL 1.4746 mL
    50 mM 0.0472 mL 0.2359 mL 0.4719 mL 1.1797 mL
    60 mM 0.0393 mL 0.1966 mL 0.3932 mL 0.9831 mL
    80 mM 0.0295 mL 0.1475 mL 0.2949 mL 0.7373 mL
    100 mM 0.0236 mL 0.1180 mL 0.2359 mL 0.5898 mL
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    ISA-2011B 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:

    ISA-2011B1395347-24-6OthersInhibitorinhibitorinhibit

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