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MedKoo CAT#: 406771
CAS#: 873305-35-2
Description: AIM-100 is a potent and selective Ack1 tyrosine kinase with IC50 value of 24 nM. AIM-100, not only inhibited Ack1 activation but also able to suppress pTyr267-AR phosphorylation, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Ack1 inhibitors hold promise for therapeutic intervention to inhibit pancreatic tumor growth.
MedKoo Cat#: 406771
Name: AIM-100
CAS#: 873305-35-2
Chemical Formula: C23H21N3O2
Exact Mass: 371.1634
Molecular Weight: 371.44
Elemental Analysis: C, 74.37; H, 5.70; N, 11.31; O, 8.61
Synonym: AIM-100; AIM 100; AIM100.
IUPAC/Chemical Name: N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenylfuro[2,3-d]pyrimidin-4-amine
InChi Key: XNFHHOXCDUAYSR-SFHVURJKSA-N
InChi Code: InChI=1S/C23H21N3O2/c1-3-8-16(9-4-1)19-20-22(24-14-18-12-7-13-27-18)25-15-26-23(20)28-21(19)17-10-5-2-6-11-17/h1-6,8-11,15,18H,7,12-14H2,(H,24,25,26)/t18-/m0/s1
SMILES Code: C12=NC=NC(NC[C@H]3OCCC3)=C1C(C4=CC=CC=C4)=C(C5=CC=CC=C5)O2
1: Mahajan K, Lawrence HR, Lawrence NJ, Mahajan NP. ACK1 tyrosine kinase
interacts with histone demethylase KDM3A to regulate the mammary tumor oncogene
HOXA1. J Biol Chem. 2014 Oct 10;289(41):28179-91. doi: 10.1074/jbc.M114.584425.
Epub 2014 Aug 22. PubMed PMID: 25148682; PubMed Central PMCID: PMC4192474.
2: Mahajan K, Coppola D, Rawal B, Chen YA, Lawrence HR, Engelman RW, Lawrence NJ,
Mahajan NP. Ack1-mediated androgen receptor phosphorylation modulates radiation
resistance in castration-resistant prostate cancer. J Biol Chem. 2012 Jun
22;287(26):22112-22. doi: 10.1074/jbc.M112.357384. Epub 2012 May 7. PubMed PMID:
22566699; PubMed Central PMCID: PMC3381169.
3: Mahajan K, Coppola D, Chen YA, Zhu W, Lawrence HR, Lawrence NJ, Mahajan NP.
Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Am
J Pathol. 2012 Apr;180(4):1386-93. doi: 10.1016/j.ajpath.2011.12.028. Epub 2012
Feb 7. PubMed PMID: 22322295; PubMed Central PMCID: PMC3349895.
4: Mahajan K, Challa S, Coppola D, Lawrence H, Luo Y, Gevariya H, Zhu W, Chen YA,
Lawrence NJ, Mahajan NP. Effect of Ack1 tyrosine kinase inhibitor on
ligand-independent androgen receptor activity. Prostate. 2010 Sep
1;70(12):1274-85. doi: 10.1002/pros.21163. PubMed PMID: 20623637; PubMed Central
PMCID: PMC3953126.