Capivasertib | AZD5363 | Akt Inhibitor | AmBeed-信号通路专用抑制剂

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Capivasertib {[allProObj[0].p_purity_real_show]}

货号：A260907 同义名： AZD5363

Capivasertib (AZD5363) 是一种口服活性和强效的泛 AKT 激酶抑制剂，对 Akt1、Akt2 和 Akt3 的 IC50 值分别为 3 nM、7 nM 和 7 nM。

Capivasertib 化学结构
CAS号：1143532-39-1

Capivasertib 3D分子结构
CAS号：1143532-39-1

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Capivasertib 纯度/质量文件产品仅供科研

货号：A260907 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

Akt 亚型比较

产品名称	Akt ↓ ↑	Akt1 ↓ ↑	Akt2 ↓ ↑	Akt3 ↓ ↑	其他靶点	纯度
Honokiol	✔				MEK	98%
PF-04691502	++++ P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM					98+%
PHT-427	+ Akt, Ki: 2.7 μM					99%+
Deguelin	✔				PI3K	99%+
TIC10 isomer	✔				ERK	98+%
Perifosine	+ Akt, IC50: 4.7 μM					98%
Miltefosine	✔				PKC,PI3K	98%
Triciribine	+ Akt, IC50: 130 nM					99%+
Uprosertib		+ Akt1, IC50: 180 nM	+ Akt2, IC50: 328 nM	++ Akt3, IC50: 38 nM		99%+
Afuresertib		++++ Akt1, Ki: 0.08 nM	++++ Akt2, Ki: 2 nM	++++ Akt3, Ki: 2.6 nM		99%+
Miransertib		++++ Akt1, IC50: 5 nM	++++ Akt2, IC50: 4.5 nM	++ Akt3, IC50: 16 nM		98+%
GSK-690693		++++ Akt1, IC50: 2 nM	+++ Akt2, IC50: 13 nM	+++ Akt3, IC50: 9 nM		99%+
AT7867		++ Akt1, IC50: 32 nM	++ Akt2, IC50: 17 nM	++ Akt3, IC50: 47 nM	PKA	99%+
AKT inhibitor VIII		++ Akt1, IC50: 58 nM	+ Akt2, IC50: 210 nM	+ Akt3, IC50: 2119 nM		98+%
MK-2206 2HCl		+++ Akt1, IC50: 8 nM	+++ Akt2, IC50: 12 nM	+ Akt3, IC50: 65 nM		99%+
Ipatasertib		++++ Akt1, IC50: 5 nM	++ Akt2, IC50: 18 nM	+++ Akt3, IC50: 8 nM		99%+
AT13148		++ Akt1, IC50: 38 nM	+ Akt2, IC50: 402 nM	++ Akt3, IC50: 50 nM	PKA	98+%
Capivasertib		++++ Akt1, IC50: 3 nM	+++ Akt2, IC50: 8 nM	+++ Akt3, IC50: 8 nM		99%+
A-674563 HCl		+++ Akt1, Ki: 11 nM			PKA	99%
CCT128930			+++ Akt2, IC50: 6 nM		PKA	98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Capivasertib 生物活性

靶点	Akt3 Akt3, IC50:8 nM Akt1 Akt1, IC50:3 nM Akt2 Akt2, IC50:8 nM
描述	AKT is the central node of PI3K/AKT/mTOR pathway. The PH domain and ATP-competitive site are the main target site for research of new compound^[1]. AK316078 is an ATP-competitive pan AKT inhibitor with IC50 values of 13, 66, 57 nM for AKT 1, 2 and 3 (measured by enzyme assays), respectively^[2]. AZD5363 on concentration of 0.3 – 10 μM effectively inhibited phosphorylation of S6 and 4E-BP1, which are the downstream of AKT, in LNCaP and BT474 cells, whereas it increased phosphorylation of AKT at both Ser473 and Thr308 like other ATP-competitive AKT inhibitors. Treatment with 3 μM AZD5363 for 2h can induce FOXO3a nuclear translocation. In cell growth inhibition assays, HER2⁺ and ER⁺ breast cancer cell lines showed most consistently sensitivity to AZD5363 (<3 μM). Oral administration of AZD5363 at 100 mg/kg twice daily resulted in 80% inhibition in HER2⁺ amplified, PIK3CA mutant BT474c xenografts. AZD5363 at 150 mg/kg twice daily caused pronounced tumor regression (129% inhibition), whereas 75 mg/kg twice daily resulted in 111% inhibition in HER2⁺ amplified, PIK3CA mutant HCC-1954 breast cancer xenograft^[3]. Several clinical trials of AZD5363, including a completed phase 2 study of treatment for invasive breast cancer, have been done (see in https://clinicaltrials.gov/).
作用机制	AZD5363 is an ATP-competitive AKT inhibitor.

Capivasertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
1%MCF7	400 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
23132/87		Growth Inhibition Assay		IC50=1.671 μM	24088382
AGS		Growth Inhibition Assay		IC50=0.552 μM	24088382
AZ521		Growth Inhibition Assay		IC50=25.448 μM	24088382

Capivasertib 动物研究

Dose

Mice (p.o.): min = 50 mg/kg^[4], max = 300 mg/kg^[3]

Administration

p.o.

Pharmacokinetics

Animal	Mice^[2]	Rats^[2]	Dogs^[2]
Administration	i.v.	i.v.	i.v.
T_1/2	0.2 h	0.5 h	1.7 h
Protein binding (free drug %)	14.3-16.7	23.5-25.1	19.2-22.9
Vd_ss	4.1 L/kg	4.0 L/kg	2.1 L/kg
CL	207 ml/min/kg (blood Cl) 6 μl/min/106 cells (hepatocyte Clint)	95 ml/min/kg (blood Cl) 32 μl/min/106 cells (hepatocyte Clint)	22 ml/min/kg (blood Cl) 10 μl/min/106 cells (hepatocyte Clint)
F	0.86	0.13	0.37

Capivasertib 参考文献

[1]Huck BR, Mochalkin I, et al. Recent progress towards clinically relevant ATP-competitive Akt inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2838-2848.

[2]Addie M, Ballard P, et al. Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases. J Med Chem. 2013 Mar 14;56(5):2059-73.

[3]Davies BR, Greenwood H, et al. Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012 Apr;11(4):873-87.

[4]Searle EJ, Telfer BA, et al. Akt inhibition improves long-term tumour control following radiotherapy by altering the microenvironment. EMBO Mol Med. 2017 Dec;9(12):1646-1659.

Capivasertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.31mL

4.66mL

2.33mL

Capivasertib 技术信息

CAS号	1143532-39-1
分子式	C₂₁H₂₅ClN₆O₂
分子量	428.915

别名	AZD5363
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 120 mg/mL(279.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

1%MCF7	400 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
23132/87		Growth Inhibition Assay		IC50=1.671 μM	24088382
AGS		Growth Inhibition Assay		IC50=0.552 μM	24088382
AZ521		Growth Inhibition Assay		IC50=25.448 μM	24088382
BT474c	0-1.35 μM	Growth Inhibition Assay	5 d	enhances the growth inhibition of AZD8931	26095475
C4-2	5 μM	Function Assay	0-24 h	induces AKTS473 and AKTT308 phosphorylation in a time dependent manner	23966621
C4-2	5 μM	Function Assay	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	1-10000 nM	Growth Inhibition Assay	0-3 d	inhibits cell viability dose dependently	23966621
C4-2	100-5000 nM	Growth Inhibition Assay	72 h	increases the fraction of cells undergoing cell death	23966621
DU145	0.5/1/10 μM	Function Assay	48 h	downregulates the phosphorylation of downstream pathway proteins in a dose-dependent manner	23258740
GTL-16		Growth Inhibition Assay		IC50=30 μM	24088382
HCC1954	0-1.35 μM	Growth Inhibition Assay	5 d	enhances the growth inhibition of AZD8931	26095475
HGC27		Growth Inhibition Assay		IC50=0.445 μM	24088382
HS746T		Growth Inhibition Assay		IC50=6.084 μM	24088382
IM95m		Growth Inhibition Assay		IC50=0.51 μM	24088382
KATO III		Growth Inhibition Assay		IC50=7.267 μM	24088382
KPL4	0-1.35 μM	Growth Inhibition Assay	5 d	enhances the growth inhibition of AZD8931	26095475
LNCaP	5 μM	Function Assay	0-24 h	induces AKTS473 and AKTT308 phosphorylation in a time dependent manner	23966621
LNCaP	5 μM	Function Assay	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	1-10000 nM	Growth Inhibition Assay	0-3 d	inhibits cell viability dose dependently	23966621
LNCaP	100-5000 nM	Growth Inhibition Assay	72 h	increases the fraction of cells undergoing cell death	23966621
LNCaP	0-1000 nM	Cell Viability Assay	0-4 d	reduced LNCaP cell viability in a dose- and time-dependent manner	23258740
MCF7	200 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
MCF7 LTED	200 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
MKN1		Growth Inhibition Assay		IC50=2.421 μM	24088382
MKN74		Growth Inhibition Assay		IC50=30 μM	24088382
MR49C	0-5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose dependent manner	25151012
MR49F	0-5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose dependent manner	25151012
NCI-H522		Growth Inhibition Assay		IC50=11.3 (±2.7) μM	24957682
NCI-H522	1/5/10 μM	Function Assay	4/24 h	increases AKT phosphorylation	24957682
NCI-N87		Growth Inhibition Assay		IC50=1.037 μM	24088382
NUGC-3		Growth Inhibition Assay		IC50=21.873 μM	24088382
NUGC-4		Growth Inhibition Assay		IC50=30 μM	24088382
OCUM-1		Growth Inhibition Assay		IC50=14.515 μM	24088382
PAMC82		Growth Inhibition Assay		IC50=30 μM	24088382
PC-3	0.5/1/10 μM	Function Assay	48 h	downregulates the phosphorylation of downstream pathway proteins in a dose-dependent manner	23258740
PC-3	10 μM	Function Assay	12 h	induces autophagy	23258740
PC-9		Growth Inhibition Assay		IC50=9.3 (±1.2) μM	24957682
PC-9	1/5/10 μM	Function Assay	4/24 h	increases AKT phosphorylation	24957682
SKBR3	0-1.35 μM	Growth Inhibition Assay	5 d	enhances the growth inhibition of AZD8931	26095475
SNU-1		Growth Inhibition Assay		IC50=5.258 μM	24088382
SNU-16		Growth Inhibition Assay		IC50=11.097 μM	24088382
SNU-216		Growth Inhibition Assay		IC50=30 μM	24088382
SNU-484		Growth Inhibition Assay		IC50=7.392 μM	24088382
SNU-5		Growth Inhibition Assay		IC50=30 μM	24088382
SNU-601		Growth Inhibition Assay		IC50=5.938 μM	24088382
SNU-620		Growth Inhibition Assay		IC50=3.384 μM	24088382
SNU-638		Growth Inhibition Assay		IC50=4.523 μM	24088382
SNU-668		Growth Inhibition Assay		IC50=6.003 μM	24088382
T74D	100 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
T74D LTED	100 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
TamR	400 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
ZR75	100 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323
ZR75 LTED	100 nM	Growth Inhibition Assay	6 d	increased drug sensitivity of 4-OHT and fulvestrant	26351323

Capivasertib {[allProObj[0].p_purity_real_show]}

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Capivasertib 质控信息

Capivasertib 生物活性

Capivasertib 细胞研究

Capivasertib 动物研究

Capivasertib 参考文献

Capivasertib 实验方案

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Capivasertib 质控信息

Capivasertib 生物活性

Capivasertib 细胞研究

Capivasertib 动物研究

Capivasertib 参考文献

Capivasertib 实验方案

Capivasertib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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临床研究

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