An ACK1/TNK2 inhibitor (IC50 = 21.58 nM); selective for ACK1/TNK2 over Abl1

AIM 100 – 10 mg

Brand:
Cayman
CAS:
873305-35-2
Storage:
-20
UN-No:
Non-Hazardous - /

AIM 100 is an inhibitor of activated Cdc42 kinase 1/tyrosine non-receptor kinase 2 (ACK1/TNK2; IC50 = 21.58 nM).{46604} 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.{46605} AIM 100 (4 mg/kg) enhances radiation-induced tumor growth reduction in an LNCaP-caAck castration-resistant prostate cancer (CRPC) mouse xenograft model.{46604}  

 

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Description

An ACK1/TNK2 inhibitor (IC50 = 21.58 nM); 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; inhibits EGF-induced increases in ATM protein levels, ACK1/TNK2 and androgen receptor phosphorylation, and pTyr267-androgen receptor binding to the ATM enhancer in LAPC4 cells at 1 μM; inhibits the growth of LNCaP and LAPC4 cells in a concentration-dependent manner and induces cell cycle arrest at the G0/G1 phase at 3 μM; enhances radiation-induced tumor growth reduction in an LNCaP-caAck CRPC mouse xenograft model at 4 mg/kg

Formal name: 5,6-diphenyl-N-[[(2S)-tetrahydro-2-furanyl]methyl]-furo[2,3-d]pyrimidin-4-amine

Synonyms: 

Molecular weight: 371.4

CAS: 873305-35-2

Purity: ≥98%

Formulation: A crystalline solid

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