A pan-Akt inhibitor
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AZD 5363

Item No. 15406

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide
CAS Number
1143532-39-1
Synonyms
  • Capivasertib
Molecular Formula
C21H25ClN6O2
Formula Weight
428.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 5 mg/mlEthanol: 1 mg/ml
λmax
219, 288 nm
SMILES
O=C(N[C@@H](CCO)C1=CC=C(Cl)C=C1)C(CC2)(N)CCN2C3=C4C(NC=C4)=NC=N3
InChi Code
InChI=1S/C21H25ClN6O2/c22-15-3-1-14(2-4-15)17(6-12-29)27-20(30)21(23)7-10-28(11-8-21)19-16-5-9-24-18(16)25-13-26-19/h1-5,9,13,17,29H,6-8,10-12,23H2,(H,27,30)(H,24,25,26)/t17-/m0/s1
InChi Key
JDUBGYFRJFOXQC-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $149

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    10 mg

    $270

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    25 mg

    $472

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    Product Description

    Akt functions as a key component in multiple signaling pathways including those related to cell proliferation, metabolism, and survival as well as angiogenesis. AZD 5363 is a pyrrolopyrimidine-derived compound that inhibits Akt by competitively binding to the kinase domain, preventing substrate phosphorylation by Akt.1 It inhibits Akt1, 2, and 3 with IC50 values of 3, 7, and 7 nM, respectively and also inhibits P70S6K and PKA with similar potency (IC50s = 6 and 7 nM, respectively).1 Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK2, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3.1 At 3 μM or less, AZD 5363 has been reported to inhibit the proliferation of 41 out of 182 solid and hematologic tumor cell lines, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations.1 Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3β, and S6 at an EC50 value of ~ 0.1 μM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Davies, B.R., Greenwood, H., Dudley, P., et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: Pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol. Cancer Ther. 11(4), 873-887 (2012).