AIM-100

Short Summary : Ack1 inhibitor

Category : Tyrosine Kinase|Ack1

Purity : 0.98

CAS Number : 873305-35-2

Formula : C23H21N3O2

Molecular Weight : 371.43

SMILE : C1CC(OC1)CNC2=C3C(=C(OC3=NC=N2)C4=CC=CC=C4)C5=CC=CC=C5

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : 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 M. Moreover, AIM-100 inhibited cell growth with GI50 values of 7 to 8 M 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.

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