AZD-5363

CAS No. 1143532-39-1

AZD-5363( AZD5363 | AZD-5363 | AZD 5363 | Capivasertib )

Catalog No. M10509 CAS No. 1143532-39-1

AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 58 In Stock
10MG 90 In Stock
25MG 154 In Stock
50MG 233 In Stock
100MG 357 In Stock
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Biological Information

  • Product Name
    AZD-5363
  • Note
    Research use only, not for human use.
  • Brief Description
    AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).
  • Description
    AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).(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. AZD5363Capivasertibhibitor MK-2206 is much less active (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.
  • 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.
  • 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.
  • Synonyms
    AZD5363 | AZD-5363 | AZD 5363 | Capivasertib
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    Akt
  • Recptor
    Akt1| Akt2| Akt3| ROCK2
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1143532-39-1
  • Formula Weight
    428.92
  • Molecular Formula
    C21H25ClN6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 86 mg/mL (200.5 mM)
  • SMILES
    O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO
  • Chemical Name
    (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Addie M, et al. J Med Chem, 2013, 26.
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