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AZD5363

(CAS No:1143532-39-1)
AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.
CAS No:1143532-39-1
Molecular Weight(MW):428.92
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 1143532-39-1
Molecular formula(MF) C21H25ClN6O2
Molecular Weight(MW): 428.92
Alias
Solubility
In vitro DMSO 86 mg/mL (200.5 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
Biological Activity
Description AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.
Features Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.
Targets
Akt1 [1]
(Cell-free assay)		 Akt2 [1]
(Cell-free assay)		 Akt3 [1]
(Cell-free assay)		 ROCK2 [1]
(Cell-free assay)
3 nM 8 nM 8 nM 56 nM
In vitro

AZD5363 is a potent Akt inhibitor with IC50 of 3 nM, 8 nM and 8 nM for Akt1, Akt2 and Akt3, respectively. [1] AZD5363 inhibits phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μM. AZD5363 inhibits the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of < 3 μM. [2] Activating mutations in PIK3CA, loss or inactivation of tumor suppressor PTEN, or HER2 amplification all are significantly predictive of responsiveness to AZD5363. Additionally, correlation is also seen between the RAS mutation status of cell lines and resistance to AZD5363. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 Growth Inhibition Assay 200 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
ZR75 Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
T74D Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
1%MCF7 Growth Inhibition Assay 400 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
MCF7 LTED Growth Inhibition Assay 200 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
ZR75 LTED Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
T74D LTED Growth Inhibition Assay 100 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
TamR Growth Inhibition Assay 400 nM 6 d increased drug sensitivity of 4-OHT and fulvestrant 26351323
HCC1954 Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
BT474c Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
KPL4 Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
SKBR3 Growth Inhibition Assay 0-1.35 μM 5 d enhances the growth inhibition of AZD8931 26095475
MR49C Growth Inhibition Assay 0-5 μM 48 h inhibits cell growth in a dose dependent manner 25151012
MR49F Growth Inhibition Assay 0-5 μM 48 h inhibits cell growth in a dose dependent manner 25151012
NCI-H522 Growth Inhibition Assay IC50=11.3 (±2.7) μM 24957682
PC-9 Growth Inhibition Assay IC50=9.3 (±1.2) μM 24957682
NCI-H522 Function Assay 1/5/10 μM 4/24 h increases AKT phosphorylation 24957682
PC-9 Function Assay 1/5/10 μM 4/24 h increases AKT phosphorylation 24957682
HGC27 Growth Inhibition Assay IC50=0.445 μM 24088382
IM95m Growth Inhibition Assay IC50=0.51 μM 24088382
AGS Growth Inhibition Assay IC50=0.552 μM 24088382
NCI-N87 Growth Inhibition Assay IC50=1.037 μM 24088382
23132/87 Growth Inhibition Assay IC50=1.671 μM 24088382
MKN1 Growth Inhibition Assay IC50=2.421 μM 24088382
SNU-620 Growth Inhibition Assay IC50=3.384 μM 24088382
SNU-638 Growth Inhibition Assay IC50=4.523 μM 24088382
SNU-1 Growth Inhibition Assay IC50=5.258 μM 24088382
SNU-601 Growth Inhibition Assay IC50=5.938 μM 24088382
SNU-668 Growth Inhibition Assay IC50=6.003 μM 24088382
HS746T Growth Inhibition Assay IC50=6.084 μM 24088382
KATO III Growth Inhibition Assay IC50=7.267 μM 24088382
SNU-484 Growth Inhibition Assay IC50=7.392 μM 24088382
SNU-16 Growth Inhibition Assay IC50=11.097 μM 24088382
OCUM-1 Growth Inhibition Assay IC50=14.515 μM 24088382
NUGC-3 Growth Inhibition Assay IC50=21.873 μM 24088382
AZ521 Growth Inhibition Assay IC50=25.448 μM 24088382
SNU-216 Growth Inhibition Assay IC50=30 μM 24088382
NUGC-4 Growth Inhibition Assay IC50=30 μM 24088382
SNU-5 Growth Inhibition Assay IC50=30 μM 24088382
GTL-16 Growth Inhibition Assay IC50=30 μM 24088382
MKN74 Growth Inhibition Assay IC50=30 μM 24088382
PAMC82 Growth Inhibition Assay IC50=30 μM 24088382
LNCaP Function Assay 5 μM 0-24 h induces AKTS473 and AKTT308 phosphorylation in a time dependent manner 23966621
C4-2  Function Assay 5 μM 0-24 h induces AKTS473 and AKTT308 phosphorylation in a time dependent manner 23966621
LNCaP Function Assay 5 μM 0-24 h inhibits phosphorylation of the distal AKT-pathway biomarkers including PRAS40, eIF4E, 4E-BP1, mTOR, and P70 S6 kinase in a time-dependent manner 23966621
C4-2  Function Assay 5 μM 0-24 h inhibits phosphorylation of the distal AKT-pathway biomarkers including PRAS40, eIF4E, 4E-BP1, mTOR, and P70 S6 kinase in a time-dependent manner 23966621
LNCaP Growth Inhibition Assay 1-10000 nM 0-3 d inhibits cell viability dose dependently 23966621
C4-2  Growth Inhibition Assay 1-10000 nM 0-3 d inhibits cell viability dose dependently 23966621
LNCaP Growth Inhibition Assay 100-5000 nM 72 h increases the fraction of cells undergoing cell death 23966621
C4-2  Growth Inhibition Assay 100-5000 nM 72 h increases the fraction of cells undergoing cell death 23966621
PC-3 Function Assay 0.5/1/10 μM 48 h downregulates the phosphorylation of downstream pathway proteins in a dose-dependent manner 23258740
DU145  Function Assay 0.5/1/10 μM 48 h downregulates the phosphorylation of downstream pathway proteins in a dose-dependent manner 23258740
LNCaP Cell Viability Assay 0-1000 nM 0-4 d reduced LNCaP cell viability in a dose- and time-dependent manner  23258740
PC-3  Function Assay 10 μM 12 h induces autophagy 23258740

... Click to View More Cell Line Experimental Data
In vivo Oral dosing of AZD5363 (100, 300 mg/kg) to nude mice causes dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts, 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 AZD5363 (130, 200, and 300 mg/kg) causes dose-dependent growth inhibition of xenografts derived from various tumor types, including HER2+ breast cancer models that are resistant to trastuzumab. AZD5363 also significantly enhances the antitumor activity of docetaxel, lapatinib, and trastuzumab in breast cancer xenografts. [2]
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