A pan-Akt inhibitor (Akt1

AZD 5363 – 5 mg

Brand:
Cayman
CAS:
1143532-39-1
Storage:
-20
UN-No:
Non-Hazardous - /

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.{25455} 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).{25455} Furthermore, AZD 5363 shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3.{25455} 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.{25455} 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.{25455}  

 

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Description

A pan-Akt inhibitor (Akt1, 2, and 3 IC50s = 3, 7, and 7 nM, respectively) that also inhibits P70S6K and PKA (IC50s = 6 and 7 nM, respectively) and shows >75% inhibition at 1 μM against ROCK-II, MKK1, MSK1, MSK2, PKCγ, PKGα, PKGβ, PRKX, RSK2, and RSK3; inhibits the proliferation of various tumor cell lines both in vitro and in vivo, demonstrating the greatest sensitivity towards breast cancer derived-cells or those with PIK3CA and/or PTEN mutations

Formal name: 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide

Synonyms: 

Molecular weight: 428.9

CAS: 1143532-39-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PKA||Product Type|Biochemicals|Kinase Inhibitors|PKB/Akt||Product Type|Biochemicals|Kinase Inhibitors|S6K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Cell Biology|Cell Signaling|cGMP Signaling

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