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

AIM-100 

Cat. No.: HY-15290 Purity: 99.95%
Handling Instructions

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.

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

AIM-100 Chemical Structure

AIM-100 Chemical Structure

CAS No. : 873305-35-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 624 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.
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    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]

    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].

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

    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].

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

    Molecular Weight

    371.43

    Formula

    C₂₃H₂₁N₃O₂

    CAS No.

    873305-35-2

    SMILES

    C1(C2=C(C3=CC=CC=C3)OC4=C2C(NC[[email protected]@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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (134.61 mM; Need ultrasonic)

    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
    10 mM 0.2692 mL 1.3461 mL 2.6923 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    AIM-100AIM100AIM 100Ack1Activated CDC42 kinase 1TNK2Tyr-phosphorylationanticancerTyr267PSANKX3.1TMPRSS2ATMInhibitorinhibitorinhibit

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    Product Name:
    AIM-100
    Cat. No.:
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