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抑制剂/激动剂
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外泌体 肿瘤生长增殖和凋亡
/ mTOR / AZD-8055

AZD-8055 {[allProObj[0].p_purity_real_show]}

货号：A224432 同义名： CCG-168

AZD-8055是一种有效、选择性且口服可用的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM，抑制mTORC1和mTORC2。

AZD-8055 化学结构 CAS号：1009298-09-2
AZD-8055 化学结构
CAS号：1009298-09-2
AZD-8055 3D分子结构
CAS号：1009298-09-2
AZD-8055 化学结构 CAS号：1009298-09-2
AZD-8055 3D分子结构 CAS号：1009298-09-2
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AZD-8055 纯度/质量文件 产品仅供科研

货号：A224432 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 mTOR ↓ mTORC1 ↓ mTORC2 ↓ 其他靶点 纯度
AZD-8055 ++++

mTOR (truncated), IC50: 0.13 nM

mTOR (full length), IC50: 0.8 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。

AZD-8055 生物活性

靶点

  • mTOR

    mTOR (truncated), IC50:0.13 nM

    mTOR (full length), IC50:0.8 nM
描述 The kinase mTOR, belonging to the PIKKs family, can form two distinct multiprotein complexes, mTORC1 and mTORC2, which regulate cell growth, cell survival, and autophagy. AZD8055 is a second generation inhibitor of mTOR with IC50 against mTOR of 0.13 nM/0.8 nM (measured with truncated recombinant mTOR enzyme and native mTOR enzyme complexes extracted from HeLa cells, respectively), showing excellent selectivity (∼1,000-fold) against all class PI3K isoforms and other PIKKs members[1]. Different from rapamycin, which may activate AKT signaling as a consequence of inhibition of the negative feedback loop downstream of mTORC1[2], treatment with AZD8055 at 0 to 1280 nM can significantly inhibit pAKT-S473, p70S6K and 4E-BP1 Thr37/46 in a dose dependent manner in HEK293 or MCF-7. This shows AZD8055 can inhibit mTORC1 and mTORC2 while preventing feedback to AKT. AZD8055 can inhibit 50% proliferation on the concentration of 53 nM in U87MG, 50 nM in A549 and 20 nM in H838. Also 1 μM AZD8055 can increase LC3-II levels in the presence of E64d/leupeptin, which shows the autophagy induced by the compound in A549 and H838 cells. In U87-MG and A549 xenografts, 10 mg/kg treatment of AZD8055 orally can induce a pharmacodynamic effect on both pS6 and pAKT-s473 (decrease to 5% after 20 min and >50% for at least 8 hours later). Consistent with that, four daily doses of 20 mg/kg AZD8055 shows the significant antiproliferative effect in that model[1].
作用机制 AZD8055 binds to the ATP binding cleft of mTOR kinase[1].

AZD-8055 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
22RV1 Growth Inhibition Assay IC50=0.70717 μM SANGER
293T 20 nM Function Assay 3 h disrupts Akt-mediated TIF-IA stability, translocation, and activity 24363449
5637 Growth Inhibition Assay IC50=1.77268 μM SANGER
639-V Growth Inhibition Assay IC50=2.42758 μM SANGER

AZD-8055 动物研究

Dose Mice20028854 (p.o.): min = 2.5 mg/kg, max = 20 mg/kg
Administration p.o.
Pharmacokinetics
Animal Dogs[3]
Dose 1 mg/kg
Administration i.g.
Cmax 228 ± 39.2 ng/ml
T1/2 4.5 ± 0.7 h
AUC 787 ± 108.5 ng/ml·h
MRT 3.1 ± 0.5 h

AZD-8055 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00999882 Cancer Advanc... 展开 >>ed Hepatocellular Carcinoma 收起 << Phase 1 Completed - Hong Kong ... 展开 >> Research Site Hong Kong, Hong Kong Korea, Republic of Research Site Seongnam, Gyeonggi-do, Korea, Republic of Research Site Seoul, Korea, Republic of 收起 <<
NCT01194193 Cancer Advanc... 展开 >>ed Solid Tumours Lymphomas 收起 << Phase 1 Withdrawn(Amendment to study c... 展开 >>ompound development programme) 收起 << - -
NCT00973076 Cancer Solid ... 展开 >>Tumors Advanced Solid Malignancies 收起 << Phase 1 Completed - Japan ... 展开 >> Research Site Tokyo, Japan 收起 <<

AZD-8055 参考文献

[1]Chresta CM, Davies BR, et al. AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res. 2010 Jan 1;70(1):288-98.

[2]Sarbassov DD, Ali SM, et al. Growing roles for the mTOR pathway. Curr Opin Cell Biol. 2005 Dec;17(6):596-603. Epub 2005 Oct 13.

[3]Liu Y, Xia Q, et al. Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity. Bioorg Med Chem. 2018 Aug 7;26(14):3992-4000.

AZD-8055 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.48mL

4.30mL

2.15mL

AZD-8055 技术信息

CAS号1009298-09-2
分子式C25H31N5O4
分子量 465.545
别名 CCG-168
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 35 mg/mL(75.18 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+35% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

Tags: AZD-8055 | 1009298-09-2 | AZD8055 | AZD 8055 | mTOR Inhibitor | PI3K/Akt/mTOR | Autophagy | Apoptosis | mTOR | Autophagy | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | AZD-8055 纯度/质量文件 | AZD-8055 亚型比较 | AZD-8055 生物活性 | AZD-8055 细胞研究 | AZD-8055 动物研究 | AZD-8055 临床数据 | AZD-8055 参考文献 | AZD-8055 实验方案 | AZD-8055 技术信息

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