AIM 100

AIM 100 is an inhibitor of activated Cdc42 kinase 1/tyrosine non-receptor kinase 2 (ACK1/TNK2, IC50 = 21.58 nM). It is selective for ACK1/TNK2 over Abl1, BTK, LCK, and LYN (IC50s = 705.9, 871.7, 432.3, and 346.7 nM, respectively), as well as a panel of 25 additional kinases. AIM 100 (1 µM) inhibits EGF-induced increases in ataxia-telangiectasia mutated kinase (ATM) protein levels, ACK1/TNK2 and androgen receptor phosphorylation, and pTyr267-androgen receptor binding to the ATM enhancer in LAPC4 cells. It inhibits the growth of LNCaP and LAPC4 cells in a concentration-dependent manner and induces cell cycle arrest at the G0/G1 phase when used at a concentration of 3 µM. AIM 100 (4 mg/kg) enhances radiation-induced tumor growth reduction in an LNCaP-caAck castration-resistant prostate cancer (CRPC) mouse xenograft model.Formal Name: 5,6-diphenyl-N-[[(2S)-tetrahydro-2-furanyl]methyl]-furo[2,3-d]pyrimidin-4-amine. CAS Number: 873305-35-2. Molecular Formula: C23H21N3O2. Formula Weight: 371.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml. lambdamax: 320 nm. SMILES: C1(NC[C@H]2OCCC2)=C(C(C3=CC=CC=C3)=C(C4=CC=CC=C4)O5)C5=NC=N1. 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. InChi Key: XNFHHOXCDUAYSR-SFHVURJKSA-N.