AZD 5363

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. 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). Furthermore, AZD 5363 shows >75% inhibition at 1 µM against ROCK2, MKK1, MSK1, MSK2, PKCgamma, PKGalpha, PKGbeta, PRKX, RSK2, and RSK3. 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. Oral dosing to nude mice bearing BT474c xenografts resulted in antitumor activity, including the reduction of the phosphorylation of PRAS40, GSK3beta, and S6 at an EC50 value of ~ 0.1 µM.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: DMF: 10 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5mg/ml, DMSO: 5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 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.