An Akt inhibitor
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A-674563

Item No. 18715

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine
CAS Number
552325-73-2
Molecular Formula
C22H22N4O
Formula Weight
358.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/mlEthanol: 10 mg/ml
λmax
245, 299 nm
SMILES
CC1=NNC(C1=C2)=CC=C2C3=CN=CC(OC[C@@H](N)CC4=CC=CC=C4)=C3
InChi Code
InChI=1S/C22H22N4O/c1-15-21-11-17(7-8-22(21)26-25-15)18-10-20(13-24-12-18)27-14-19(23)9-16-5-3-2-4-6-16/h2-8,10-13,19H,9,14,23H2,1H3,(H,25,26)/t19-/m0/s1
InChi Key
BPNUQXPIQBZCMR-IBGZPJMESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $54

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    1 mg

    $102

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    5 mg

    $367

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    10 mg

    $627

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    Product Description

    A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki = 11 nM for Akt1).1 It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families.1 A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4 µM.1 In vivo, 40 mg/kg/day A-674563 in combination with 15 mg/kg/day paclitaxel (Item No. 10461) was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Luo, Y., Shoemaker, A.R., Liu, X., et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol. Cancer Ther. 4(6), 977-968 (2005).