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[CAS NO. 873305-35-2] AIM-100
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15290 |
| Brand: | MCE |
| CAS: | 873305-35-2 |
Overview
| MDL | MFCD22417088 |
|---|---|
| Molecular Weight | 371.43 |
| Molecular Formula | C23H21N3O2 |
| SMILES | C1(C2=C(C3=CC=CC=C3)OC4=C2C(NC[C@@H]5CCCO5)=NC=N4)=CC=CC=C1 |
3 Publications Citing Use of MCE
Summary
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 Tyr
267
phosphorylation and its recruitment to the ataxia-telangiectasia mutated kinase (ATM) enhancer
[2]
.
AIM-100 is able to suppress pTyr
267
-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.
Appearance
Solid
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
DMSO : 50 mg/mL ( 134.61 mM ; Need ultrasonic)
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 |
References
- [1] Mahajan K, et al. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Am J Pathol. 2012 Apr;180(4):1386-93.
- [2] Mahajan K, et al. Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer. J Biol Chem. 2012 Jun 22;287(26):22112-22.
- [3] Mahajan K, et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate. 2010 Sep 1;70(12):1274-85.
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