ChemicalBook > CAS DataBase List > AZD5363
AZD5363
AZD5363
- CAS No.1143532-39-1
- Chemical Name:AZD5363
- CBNumber:CB12650349
- Molecular Formula:C21H25ClN6O2
- Formula Weight:428.92
- MOL File:1143532-39-1.mol
AZD5363 Property
- Melting point 161-164°C
- Density 1.381
- storage temp. Refrigerator
- solubility DMSO (Slightly), Methanol (Slightly)
- pka 13.93±0.50(Predicted)
- form Solid
- color Off-White to Pale Beige
- FDA UNII WFR23M21IE
- NCI Drug Dictionary capivasertib
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P305+P351+P338
AZD5363 Chemical Properties,Usage,Production
- 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.
AZD5363 Preparation Products And Raw materials
Raw materials
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1143532-39-1, AZD5363Related Search:
- API
- Inhibitors
- PI3K/Akt/mTOR
- PI3K
- mTOR
- Akt
- 信号转导通路激酶抑制剂
- 原料药
- 医药原料药-原料药
- 药靶配体
- 合成有机化合物配体
- 优势产品目录
- 生物化工
- 黄金产品
- 原料药中间体
- 细胞生物学试剂
- 小分子抑制剂,天然产物
- 抑制剂
- 小分子抑制剂
- C21H25ClN6O2
- AZD5363 (CAPIVASERTIB) |CAS 1143532-39-1
- AKT激酶抑制剂(AZD5363)
- 化合物CAPIVASERTIB,10 MM DMSO 溶液
- 卡匹色替AZD5363
- 卡帕塞替尼/卡匹色替
- 卡匹色替
- AZD5363,泛泛AKT抑制剂
- 卡帕塞替尼
- (S)-1-(7H-吡咯并[2,3-D]嘧啶-4-基)-4-氨基-N-[1-(4-氯苯基)-3-羟基丙基]哌啶-4-甲酰胺
- (S)-4-氨基-N-(1-(4-氯苯基)-3-羟丙基)-1-(7H-吡咯并[2,3-D]嘧啶-4-基)哌啶-4-甲酰胺
- AKT亚型抑制剂
- AZD5363 ; AZD-5363 ; AZD 5363 ; CAPIVASERTIB
- 化合物CAPIVASERTIB
- AZD5363 抑制剂
- AZD5363, 一种有效的 PAN-AKT 激酶抑制剂
- 4-氨基-N-[(1S)-1-(4-氯苯基)-3-羟基丙基]-1-(7H-吡咯并[2,3-D]嘧啶-4-基)-4-哌啶甲酰胺
- 1143532-39-1
- Capivasertinib
- Capivasertib, 10 mM in DMSO
- Autophagy,AZD 5363,Inhibitor,inhibit,AZD-5363,PKB,Akt,Capivasertib,Protein kinase B
- Capivasertib AZD5363 AZD-5363
- (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
- Capivasertib
- 4-Piperidinecarboxamide, 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-
- AZD5363 USP/EP/BP
- 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
- AZD-5363; AZD 5363
- CS-561
- CAPIVASERTIB (AZD5363)
- AZD5363(Capivasertib)
- AZD5636
- 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
- AZD5363;AZD-5363;AZD 5363
- AZD 5363 dihydrochloride
- 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide AZD5363
- 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide
- AZD5363