AZD-5363

Name: AZD-5363
SKU: A9601
Availability: InStock

Product ID A9601

Cas No. 1143532-39-1

Purity ≥99%, ≥99%ee

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Description

AZD-5363 is an oral pan-AKT inhibitor that causes hyperphosphorylation of AKT, locking it in a catalytically inactive state, unable to phosphorylate downstream signaling substrates such as PRAS40 and GSK-β. This compound displays anticancer chemotherapeutic activity, inhibiting proliferation and inducing tumor regression in in vitro and in vivo models of HER2+ breast cancer and prostate cancer. AZD-5363 may also exhibit inhibitory activity against Rho-associated protein kinase (ROCK), p70S6K, PKA, MKK1, MSK1, MSK2, PKC, PKG, PRKX, and RSK2/3.

Product Info

Cas No.	1143532-39-1
Purity	≥99%, ≥99%ee
Formula	C₂₁H₂₅ClN₆O₂
Formula Wt.	428.92
Chemical Name	4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)piperidine-4-carboxamide
IUPAC Name	4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)piperidine-4-carboxamide
Synonym	AZD5363
Solubility	In DMSO(86mg/ml), water with 2 eq. of acid, insoulble on ethanol
Appearance	White Crystal Powder

Shipping and Storage

Store Temp	-20°C
Ship Temp	Ambient

Downloads

MSDS	A9601 MSDS PDF
Info Sheet	A9601 Info Sheet PDF
Brochures	PI3K-Akt-mTORC Pathway Booklet

References

Addie M, Ballard P, Buttar D, 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 Mar 14;56(5):2059-73. PMID: 23394218.

Lamoureux F, Thomas C, Crafter C, et al. Blocked autophagy using lysosomotropic agents sensitizes resistant prostate tumor cells to the novel Akt inhibitor AZD5363. Clin Cancer Res. 2013 Feb 15;19(4):833-44. PMID: 23258740.

Davies BR, 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. 2012 Apr;11(4):873-87. PMID: 22294718.

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AZD-5363

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