| Identification | Back Directory | [Name]
AZD5363 | [CAS]
1143532-39-1 | [Synonyms]
CS-561
AZD5636
AZD5356
AZD5363
Capivasertib
AZD5363 USP/EP/BP
AZD-5363; AZD 5363
AZD5363(Capivasertib)
CAPIVASERTIB (AZD5363)
AZD 5363 dihydrochloride
AZD5363;AZD-5363;AZD 5363
AZD5363, 99%, a potent pan-AKT kinase inhibitor
(S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidi
4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide
4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
4-Piperidinecarboxamide, 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-
4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide AZD5363 | [Molecular Formula]
C21H25ClN6O2 | [MDL Number]
MFCD22628785 | [MOL File]
1143532-39-1.mol | [Molecular Weight]
428.92 |
| Chemical Properties | Back Directory | [Melting point ]
161-164°C | [density ]
1.381 | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
13.93±0.50(Predicted) | [color ]
Off-White to Pale Beige |
| Hazard Information | Back Directory | [Uses]
AZD5363 is used in inhibiting the proliferation of certain tumor cell lines. | [Biological Activity]
azd5363 is a novel, potent phosphoinositide 3-kinase (pi3k)/akt pathway inhibitor with ic50 value of ~200nm. [1]azd5363 is proved to inhibit castrate resistant prostate cancer (crpc) progression. clusterin (clu) and autophagy will be induced which may work as cytoprotective responses which can affect the downstream pi3k/akt signaling. [2] azd5363 inhibits the growth of a lot of human tumor cells in a dose dependent manner. the mode of action could be monotherapy as well as in combination with her2 inhibitors in breast cancer models. [3] it is suggested to induce cell apoptosis by measuring the expression of parp cleavage, the activity of caspase 3, et al. [1]most importantly, azd5363 can target the pi3k/akt-pathway in vivo significantly, thus reducing the serum psa-levels and tumor volume, finally, it could postpone the progression to crpc.[1] | [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[1]. | [target]
Akt | [IC 50]
Akt1: 3 nM (IC50); Akt2: 7 nM (IC50); Akt3: 7 nM (IC50); P70S6K: 6 nM (IC50); PKA: 7 nM (IC50); ROCK2: 60 nM (IC50); ROCK1: 470 nM (IC50); Autophagy | [storage]
Store at -20°C | [References]
[1] thomas c, crafter c, davies b, zoubeidi a, gleave me. azd5363, a novel akt inhibitor, delays prostate cancer progression. the journal of urology. may 2011. 185(4s): e292-293.
[2] kumano m, zhang f, shiota m, crafter c, davies b, zoubeidi a, gleave m. clusterin knockdown enhances antitumor activity of a novel akt inhibitor, azd5363, through inhibition of autophagy in prostate cancer. the journal of urology. may 21 2012. e392.
[3] davies br, greenwood h, dudley p, et al. preclinical pharmacology of azd5363, an inhibitor of akt: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. mol. cancer ther. arp 2012. 11: 873. |
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