Vistusertib | AZD2014 | mTORC Inhibitor | AmBeed-信号通路专用抑制剂

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Vistusertib 99%+

货号：A386287 同义名： AZD2014

Vistusertib（AZD2014）是一种ATP竞争性mTOR抑制剂，IC50为2.81 nM，抑制mTORC1和mTORC2复合物。

Vistusertib 化学结构
CAS号：1009298-59-2

Vistusertib 3D分子结构
CAS号：1009298-59-2

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Vistusertib 纯度/质量文件产品仅供科研

货号：A386287 标准纯度： 99%+ 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

mTOR 亚型比较

产品名称	mTOR ↓ ↑	mTORC1 ↓ ↑	mTORC2 ↓ ↑	其他靶点	纯度
AZD-8055	++++ mTOR (full length), IC50: 0.8 nM mTOR (truncated), IC50: 0.13 nM				99%+
Gedatolisib	++++ mTOR, IC50: 1.6 nM				98%
GSK1059615	++ mTOR, IC50: 12 nM				98%
Vistusertib	+++ mTOR, IC50: 2.8 nM				99%+
Torin 1	+++ mTOR, IC50: 4.32 nM	+++ mTORC1, IC50: 2 nM	++ mTORC2, IC50: 10 nM	DNA-PK	99%+
Dactolisib	+++ mTOR (p70S6K), IC50: 6 nM				98+%
PI-103	+ mTOR, IC50: 30 nM				99%+
WAY-600	++ mTOR, IC50: 9 nM				99%
Voxtalisib	+ mTOR, IC50: 157 nM				99%+
PF-04691502	++ mTOR, Ki: 16 nM				98+%
Onatasertib	++ mTOR, IC50: 16 nM			DNA-PK	99%+
Chrysophanol	✔			EGFR	98%
Samotolisib	✔			DNA-PK	99%+
Torkinib	+++ mTOR, IC50: 8 nM			PDGFR,DNA-PK	99%+
Everolimus					99%+
WYE-354	+++ mTOR, IC50: 5 nM				98%
Tacrolimus	✔				98%
PP121	++ mTOR, IC50: 13 nM			PDGFR,VEGFR	99%+
Torin 2	++++ mTOR, IC50: 0.25 nM			DNA-PK	99%+
Rapamycin	++++ mTOR, IC50: ~0.1 nM				98%
GDC-0349	+++ mTOR, Ki: 3.8 nM				98%
XL388	++ mTOR, IC50: 9.9 nM	+++ mTORC1, IC50: 8 nM	+ mTORC2, IC50: 166 nM		99%+
WYE-687	+++ mTOR, IC50: 7 nM				98+%
Apitolisib	+ mTOR, Ki app: 17 nM				98%+
WYE-132	++++ mTOR, IC50: 0.19 nM				99%+
Sapanisertib	++++ mTOR, Ki: 1.4 nM				99%+
BGT226 maleate	✔				99%+
ETP-46464	++++ mTOR, IC50: 0.6 nM			DNA-PK	98%
PI3K-IN-1	+ mTOR, IC50: 157 nM				98+%
Zotarolimus	+++ FKBP-12, IC50: 2.8 nM				99+%
OSI-027	+++ mTOR, IC50: 4 nM	+ mTORC1, IC50: 22 nM	+ mTORC2, IC50: 65 nM		99%+
Ridaforolimus	++++ mTOR, IC50: 0.2 nM				99%+
Temsirolimus	+ mTOR, IC50: 1.76 μM				99%
CZ415	++ mTOR, pIC50: 8.07				99%+
SF2523	+ mTOR, IC50: 280 nM			DNA-PK	99%+
KU-0063794		++ mTORC1, IC50: ~10 nM	++ mTORC2, IC50: ~10 nM		99%+
Omipalisib		++++ mTORC1, Ki: 0.18 nM	++++ mTORC2, Ki: 0.3 nM		99%+
Palomid 529		✔			99%+
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。

Vistusertib 生物活性

靶点	mTOR mTOR, IC50:2.8 nM
描述	The kinase mTOR, belonging to the PIKKs family, which regulate cell growth, cell survival, and autophagy, is a key target in the development of antitumor therapies. It was found that rapamycin and its analogues, the first generation of mtor inhibitor, can activate AKT signaling as a consequence of inhibition of the negative feedback loop downstream of mTORC1. AZD2014 (Vistusertib) is a potent mTORC1/2 inhibitor (IC50 = 2.8 nM, measured by recombinant truncated FLAG-tagged mTOR) and displays a high level of selectivity against other members of the PIKKs [a]. Different from rapamycin, treatment with AZD2014 at 3 to 1000 nM can significantly inhibit mTOR substrates, such as pS6-S235/236, p70S6K-T389 and 4E-BP1 Thr37/46, in a dose dependent manner, as well as no AKT activation, in MCF7 cells. While effectively inhibiting signaling to S6, PRAS40 as well as feedback phosphorylation of AKT, AZD2014 can block proliferation in all cell lines, including everolimus-resistant cells and long-term estrogen-deprived (LTED) everolimus-resistant cells at concentration 200/500 nM. Treatment of 15 mg/kg AZD2014 can induce significant growth inhibition in several hormone therapy–sensitive ERb breast cancer xenograft models like MCF7 and HCC1500, as well as three patient-derived primary explant models BR0555, CTC174, and HBCx3. Up to now, AZD2014 enters Phase 1 trial in solid tumours^[1].
作用机制	AZD2014 is a small-molecule ATP competitive inhibitor of mTOR^[2]

Vistusertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay		Inhibition of recombinant FLAG-tagged mTOR (1362 to 2549) (unknown origin) expressed in HEK293 cells, IC50=2.8 nM	23375793
human MCF7 cells		Function assay		Inhibition of mTORC1 in human MCF7 cells xenografted mouse assessed as modulation substrate	23375793
human MDA-MB-468 cells		Function assay	2 h	Inhibition of mTORC2 in human MDA-MB-468 cells assessed as reduction of AKT phosphorylation at Ser473 after 2 hrs, IC50=0.08 μM	23375793
human MDA-MB-468 cells		Function assay	2 h	Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction of pS6 phosphorylation at Ser235/236 after 2 hrs, IC50=0.2 μM	23375793

Vistusertib 动物研究

Dose

Mice^[3] (p.o.): min = 3.75 mg/kg, max = 20 mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Mice^[3]
Dose	20 mg/kg
Administration	s.c.
C_max	15 μmol/L
AUC	4320 μmol/L·h

Vistusertib 参考文献

[1]First-in-human phase I trial of the dual mTORC1 and mTORC2 inhibitor AZD2014 in solid tumors.

[2]Pike KG, Malagu K, et al. Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1212-6.

[3]Guichard SM, Curwen J, et al. AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules. Mol Cancer Ther. 2015 Nov;14(11):2508-18.

Vistusertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.81mL

2.16mL

1.08mL

21.62mL

4.32mL

2.16mL

Vistusertib 技术信息

CAS号	1009298-59-2
分子式	C₂₅H₃₀N₆O₃
分子量	462.544

别名	AZD2014
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(108.1 mM)，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+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Vistusertib 99%+

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Vistusertib 质控信息

Vistusertib 生物活性

Vistusertib 细胞研究

Vistusertib 动物研究

Vistusertib 参考文献

Vistusertib 实验方案

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Vistusertib 99%+

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Vistusertib 质控信息

Vistusertib 生物活性

Vistusertib 细胞研究

Vistusertib 动物研究

Vistusertib 参考文献

Vistusertib 实验方案

Vistusertib 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

细胞研究

临床研究

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