2. Protein Tyrosine Kinase/RTK
  3. Ack1
  4. AIM-100

AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect.

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AIM-100 Chemical Structure

AIM-100 Chemical Structure

CAS No. : 873305-35-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 132 In-stock
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10 mM * 1 mL in DMSO USD 132 In-stock
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10 mg USD 130 In-stock
50 mg USD 460 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

AIM-100 Related Antibodies

Top Publications Citing Use of Products

    AIM-100 purchased from MedChemExpress. Usage Cited in: Mol Med. 2023 Jan 16;29(1):6.  [Abstract]

    AIM-100 (10, 20 µM; 24, 48, 72 h) significantly decreases A549 cell proliferation.

    AIM-100 purchased from MedChemExpress. Usage Cited in: Mol Med. 2023 Jan 16;29(1):6.  [Abstract]

    AIM-100 (10, 20 µM; 72 h) significantly reduces the colony formation of A549 cells.

    AIM-100 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Dec 1;6(38):40622-41.  [Abstract]

    Ack1 Affects Ser473-phosphorylation of AKT, but not Thr308-phosphorylation in HCC Cells. A. & B. HCC cells are either untreated or pretreated with AIM-100, a Ack1-specific inhibitor, in cell adhesion assays. Upon AIM- 100 treatment, significant loss of p-Ack1 level and a concomitant decrease in Ser473-phosphorylation of AKT level is observed, whereas the effect on Thr308-phosphorylation of AKT levels is not altered.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect[1][2].

    IC50 & Target

    IC50: 21.58 nM (Ack1)[2]
    Cellular Effect
    Cell Line Type Value Description References
    LNCaP IC50
    7 μM
    Compound: 1b, AIM-100
    Anticancer activity against human LNCAP cells assessed as inhibition of cell growth after 72 hrs by trypan blue exclusion assay
    Anticancer activity against human LNCAP cells assessed as inhibition of cell growth after 72 hrs by trypan blue exclusion assay
    		[PMID: 25699576]
    In Vitro

    AIM-100 (2-10 μM; 48 hours) treatment not only inhibits Ack1 activation but also suppresses AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 phase. AIM-100 not only inhibits Ack1/AKT Tyr-phosphorylation but also suppressed growth of cell lines derived from pancreatic, breast, and lung tumors[1].
    The Ack1 inhibitor AIM-100 not only inhibited Ack1 activity but also was able to suppress AR Tyr267 phosphorylation and its recruitment to the ataxia-telangiectasia mutated kinase (ATM) enhancer[2].
    AIM-100 is able to suppress pTyr267-AR phosphorylation, binding of androgen receptor (AR) to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity[3].

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

    AIM-100 Related Antibodies
    In Vivo

    In male nude castrated mice, AIM-100 (4 mg/kg) suppresses growth of radioresistant castration-resistant prostate cancer (CRPC) xenograft tumors by decreasing ataxia-telangiectasia mutated kinase (ATM) expression[2].

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

    371.43

    Formula

    C23H21N3O2
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    C1(C2=C(C3=CC=CC=C3)OC4=C2C(NC[C@@H]5CCCO5)=NC=N4)=CC=CC=C1
    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 : 50 mg/mL (134.61 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 2.6923 mL 13.4615 mL 26.9230 mL
    5 mM 0.5385 mL 2.6923 mL 5.3846 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
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    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 (6.73 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 (6.73 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.
    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
    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 2.6923 mL 13.4615 mL 26.9230 mL 67.3074 mL
    5 mM 0.5385 mL 2.6923 mL 5.3846 mL 13.4615 mL
    10 mM 0.2692 mL 1.3461 mL 2.6923 mL 6.7307 mL
    15 mM 0.1795 mL 0.8974 mL 1.7949 mL 4.4872 mL
    20 mM 0.1346 mL 0.6731 mL 1.3461 mL 3.3654 mL
    25 mM 0.1077 mL 0.5385 mL 1.0769 mL 2.6923 mL
    30 mM 0.0897 mL 0.4487 mL 0.8974 mL 2.2436 mL
    40 mM 0.0673 mL 0.3365 mL 0.6731 mL 1.6827 mL
    50 mM 0.0538 mL 0.2692 mL 0.5385 mL 1.3461 mL
    60 mM 0.0449 mL 0.2244 mL 0.4487 mL 1.1218 mL
    80 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 mL
    100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6731 mL
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    AIM-100 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:

    AIM-100873305-35-2AIM100AIM 100Ack1Activated Cdc42 kinase 1TNK2Tyr-phosphorylationanticancerTyr267PSANKX3.1TMPRSS2ATMInhibitorinhibitorinhibit

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