AZD-5363

SKU: orb1226921

Description

AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 30 μM).(In Vivo):Oral dosing of Capivasertib (AZD5363) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50 ~0.1 μM total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts.

Key Properties

• CAS Number: 1143532-39-1
• MW: 428.92
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₅ClN₆O₂
• SMILES: O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO
• Target: Akt
• Solubility: DMSO: 86 mg/mL (200.5 mM)

Bioactivity

• In Vivo:
  Oral dosing of Capivasertib (AZD5363) to nude mice causes dose-and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC50 ~0.1 μM total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose (18F-FDG) uptake in U87-MG xenografts. Chronic oral dosing of Capivasertib caused dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models. Capivasertib also significantly enhances the antitumor activity of RP-56976 and GW572016 in breast cancer xenografts.
• In Vitro:
  Capivasertib, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms with a potency of 10 nM or less. Capivasertib inhibits phosphorylation of these substrates with an IC50 value of 0.06 to 0.76 μM in the 3 cell lines. Capivasertib effectively inhibits phosphorylation of S6 and 4E-BP1 in these cell lines, whereas it increases phosphorylation of AKT at both ser473 and thr308. In BT474c cells, Capivasertib induces FOXO3a nuclear translocation with EC50 value of 0.69 μM; a concentration of 3 μM is sufficient to almost completely localize FOXO3a to the nucleus.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD5363 | AZD-5363 | AZD 5363 | Capivasertib

Quick Database Links

Gene Symbol

Akt