AZD-5363 Inhibitor CAS No. 1143532-39-1

Cat. No.	Name	Size	Price	Add Cart
KI2774	AZD-5363	5 mg	$234
KI2774	AZD-5363	25 mg	$752

Chemical Characteristic

Product Name	AZD-5363
Synonyms	AZD5363
CAS No.	1143532-39-1
Molecular Weight	428.92
Formula	C₂₁H₂₅ClN₆O₂
Chemical Name	4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
Smiles	N1(CCC(CC1)(C(=O)NC(CCO)c1ccc(cc1)Cl)N)c1c2c(ncn1)[nH]cc2
Chemical Structure

Biological activities

AZD-5363 is a potent and selective inhibitor of AKT. AZD-5363 inhibits all isoforms of Akt(Akt1,Akt2 and Akt3) with IC50s of 3,8 and 8 nM, respectively.^[1] AZD-5363 inhibits the AKT downstream pathway by reducing p-MTOR and p-RPS6KB/p70S6K.^[2] In vitro, AZD-5363 inhibits the proliferation of LNCaP prostate cancer cells and BT474c breast adenocarcinoma cells with a potency of 3 μM or less. In vivo, AZD-5363 significantly enhances the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts.[3]

Protocols

In vitro, AZD-5363 is dissolved in DMSO.^[3]

References

[1] Addie M, et al. Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases. J Med Chem. 2013, 56(5):2059-2073. [2] Lamoureux F, et al. Dual inhibition of autophagy and the AKT pathway in prostate cancer. Autophagy. 2013, 9(7):1119-1120. [3] Davies BR, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012, 11 (4): 873-887.

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