ChemicalBook > CAS DataBase List > Capivasertib

Capivasertib

Product Name: Capivasertib
CAS No.: 1143532-39-1
Chemical Name: Capivasertib
Synonyms: Capivasertib;4-Piperidinecarboxamide, 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-;CS-561;AZD5636;AZD5363;AZD5356;Capivasertinib;AZD5363 USP/EP/BP;AZD-5363; AZD 5363;AZD5363(Capivasertib)
CBNumber: CB12650349
Molecular Formula: C21H25ClN6O2
Formula Weight: 428.92
MOL File: 1143532-39-1.mol

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Capivasertib 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
InChIKey: JDUBGYFRJFOXQC-KRWDZBQOSA-N
SMILES: N1(C2N=CN=C3NC=CC3=2)CCC(N)(C(N[C@H](C2=CC=C(Cl)C=C2)CCO)=O)CC1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 15406
Product name: AZD 5363
Purity: ≥98%
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 15406
Product name: AZD 5363
Purity: ≥98%
Packaging: 5mg
Price: $166
Updated: 2024/03/01

Cayman Chemical

Product number: 15406
Product name: AZD 5363
Purity: ≥98%
Packaging: 10mg
Price: $231
Updated: 2024/03/01

Cayman Chemical

Product number: 15406
Product name: AZD 5363
Purity: ≥98%
Packaging: 25mg
Price: $412
Updated: 2024/03/01

Tocris

Product number: 6978
Product name: AZD5363
Purity: ≥98%(HPLC)
Packaging: 25
Price: $545
Updated: 2021/12/16

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Capivasertib 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]

Synthesis

1143534-59-1

3680-69-1

1143532-39-1

General steps: 1. N,N-diisopropylethylamine (1.676 mL, 9.62 mmol) was added under nitrogen protection to a solution containing (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)piperidine-4-carboxamide (Intermediate 49) (1 g, 3.21 mmol) and 4-chloro-7H-pyrrolo[2,3-d]pyrimidine (0.493 g 3.21 mmol) in a solution of n-butanol (15 mL). 2. The reaction mixture was stirred at 60 °C for 18 hours. 3. After completion of the reaction, the reaction mixture was diluted with ethyl acetate (50 mL) and washed sequentially with water (25 mL) and saturated saline (25 mL). 4. The organic layer was separated, dried with anhydrous magnesium sulfate, filtered and concentrated under reduced pressure to obtain the crude product. 5. The crude product was purified by fast silica gel column chromatography using dichloromethane with a gradient elution containing 0 to 6% methanol and ammonia. 6. The purified fraction was collected and concentrated to dryness under reduced pressure to afford (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (842 mg) as a white foamy solid. 7. The resulting product was dissolved in ethyl acetate (7 mL) and stirred for 18 hours. 8. The precipitated solid was collected by filtration, washed with a small amount of ethyl acetate and dried in a vacuum oven at 55 °C for 18 h. (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (0.585 g, 42.5% yield) was obtained as a white solid. Mass spectrum (electrospray positive ion mode): m/z (ES+) (M + H)+ = 429; HPLC retention time tR = 1.60 min. 1H NMR (400.13 MHz, DMSO-d6) δ 1.39-1.47 (2H, m), 1.80-2.02 (4H, m), 2.17 (2H, s), 3.35-3.40 (2H, m), 3.50-3.59 (2H, m), 4.34-4.41 (2H, m), 4.53 (1H, t), 4.88 (1H, d), 6.57 (1H, m), 7.14-7.16 (1H, m), 7.31-7.37 (4H, m), 8.12 (1H, s), 8.42 (1H, d), 11.62 (1H, s).

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.

Capivasertib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Capivasertib manufacturers

Apeloa production Co.,Limited

Product: Capivasertib (AZD5363) 1143532-39-1
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 11000
Release date: 2024-06-17

Career Henan Chemical Co

Product: AZD5363 1143532-39-1
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

1143532-39-1, CapivasertibRelated Search:

2-amino-4-chlorobenzamide 2-Amino-5-chlorobenzophenone Everolimus 4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol MK-2206 2HCl GDC-0068 Trametinib Rapamycin

AZD5356

AZD5363

4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide

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

AZD 5363 dihydrochloride

AZD5363;AZD-5363;AZD 5363

(S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidi

Capivasertib

AZD5363, 99%, a potent pan-AKT kinase inhibitor

AZD5636

AZD5363(Capivasertib)

CAPIVASERTIB (AZD5363)

CS-561

AZD-5363; AZD 5363

4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

AZD5363 USP/EP/BP

(S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide

Capivasertib AZD5363 AZD-5363

Autophagy,AZD 5363,Inhibitor,inhibit,AZD-5363,PKB,Akt,Capivasertib,Protein kinase B

Capivasertib, 10 mM in DMSO

Capivasertinib

1143532-39-1

C21H25ClN6O2

Inhibitors

Akt

mTOR

PI3K

PI3K/Akt/mTOR

API