
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)






Size | Price / USD | Stock | Quantity |
2MG | 41 | In Stock |
![]() ![]() |
5MG | 58 | In Stock |
![]() ![]() |
10MG | 90 | In Stock |
![]() ![]() |
25MG | 154 | In Stock |
![]() ![]() |
50MG | 233 | In Stock |
![]() ![]() |
100MG | 357 | In Stock |
![]() ![]() |
200MG | Get Quote | In Stock |
![]() ![]() |
500MG | Get Quote | In Stock |
![]() ![]() |
1G | Get Quote | In Stock |
![]() ![]() |
Biological Information
-
Product NameAZD-5363
-
NoteResearch use only, not for human use.
-
Brief DescriptionAZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).
-
DescriptionAZD5363, 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 VitroCapivasertib, 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 VivoOral 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.
-
SynonymsAZD5363 | AZD-5363 | AZD 5363 | Capivasertib
-
PathwayPI3K/Akt/mTOR signaling
-
TargetAkt
-
RecptorAkt1| Akt2| Akt3| ROCK2
-
Research AreaCancer
-
Indication——
Chemical Information
-
CAS Number1143532-39-1
-
Formula Weight428.92
-
Molecular FormulaC21H25ClN6O2
-
Purity>98% (HPLC)
-
SolubilityDMSO: 86 mg/mL (200.5 mM)
-
SMILESO=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℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1.Addie M, et al. J Med Chem, 2013, 26.
molnova catalog



related products
-
Ipatasertib
Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor.
-
Lupeol
Lupeol is a pentacyclic triterpene that has anti-inflammatory and antioxidant activity.
-
Perifosine
A oral bioavailable alkylphospholipid that displays significant antiproliferative activity in vitro and in vivo in several human tumor model; acts as an Akt inhibitor and a PI3K inhibitor.