| AIM-100Ack1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.72%
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| Cas No. | 873305-35-2 | SDF | Download SDF |
| Synonyms | AIM 100;AIM100 | ||
| Chemical Name | N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenylfuro[2,3-d]pyrimidin-4-amine | ||
| Canonical SMILES | C1CC(OC1)CNC2=C3C(=C(OC3=NC=N2)C4=CC=CC=C4)C5=CC=CC=C5 | ||
| Formula | C23H21N3O2 | M.Wt | 371.43 |
| Solubility | ≥36 mg/mL in DMSO with gentle warming, <1.83 mg/ml="" in="" h2o,="" ≥35.8="" mg/ml="" in="" etoh="" with="" gentle="" warming=""> | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AIM-100 is a small inhibitor of Ack1 tyrosine kinase with IC50 value of 24 nM [1].
AIM-100 mimicked ATP and inhibited the activity of Ack1 significantly and specifically. It showed no inhibition activity for the other 30 kinases including PI3-kinase and AKT, and showed a five-fold higher IC50 value for Lck. In MEF cells treated with EGF, AIM-100 caused a remarkable decrease of the activation of Ack1. In the human prostate cancer cells LNCaP and LAPC4, AIM-100 treatment resulted in an increase of G0/G1 cell phase and subsequent cell growth suppression. These effects of AIM-100 also exerted in the pancreatic cancer cells. AIM-100 induced apoptosis in Panc-1 cells at concentration of 10 μM. Moreover, AIM-100 inhibited cell growth with GI50 values of 7 to 8 μM in CD-18, Panc-1, OV90, MCF-7 and MDA-MB-468 cancer cells [1, 2].
References:1. Mahajan K, Challa S, Coppola D, et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. The Prostate, 2010, 70(12): 1274-1285. 2. Mahajan K, Coppola D, Chen Y, et al. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. The American journal of pathology, 2012, 180(4): 1386-1393.
