An ACK1/TNK2 inhibitor
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AIM 100

Item No. 29487

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 16 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $183

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    25 mg

    $378

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    50 mg

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    Product Description

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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mahajan, K., Coppola, D., Rawal, B., et al. Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer. The Journal of Biological Chemisty 287(26), 22112-22122 (2012).

    2. Mahajan, K., Challa, S., Coppola, D., et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate 70(12), 1274-1285 (2010).