Sapanisertib | INK-128 | mTOR1/2 Inhibitor | AmBeed-信号通路专用抑制剂

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沙帕色替 /Sapanisertib {[allProObj[0].p_purity_real_show]}

货号：A121801 同义名： INK-128;TAK-228

Sapanisertib (INK-128; MLN0128; TAK-228) 是一种口服可用的ATP依赖性mTOR1/2抑制剂，对mTOR激酶的IC50为1 nM。

Sapanisertib 化学结构
CAS号：1224844-38-5

Sapanisertib 3D分子结构
CAS号：1224844-38-5

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Sapanisertib 纯度/质量文件产品仅供科研

货号：A121801 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

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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。

Sapanisertib 生物活性

靶点	mTOR mTOR, Ki:1.4 nM
描述	Sapanisertib (INK-128) demonstrates enzymatic inhibitory activity against mTOR with over 100-fold selectivity compared to PI3K kinases^[1]. Sapanisertib (INK-128) selectively reduces the protein levels of YB1, MTA1, vimentin, and CD44 without affecting their mRNA levels in PC3 cells. It also diminishes the invasive capabilities of PC3 prostate cancer cells. Additionally, Sapanisertib (INK-128) impedes cancer cell migration beginning at 6 hours post-treatment, coinciding with the evident reduction in pro-invasion gene expression, and before any alterations in the cell cycle or overall global protein synthesis are observed^[2].
体内研究	In a ZR-75-1 breast cancer xenograft model, Sapanisertib (INK-128) effectively inhibits tumor growth at a daily dose of 0.3 mg/kg^[1]. Treatment with INK128 fully restores 4EBP1 and p70S6K1/2 phosphorylation to wild-type levels in PtenL/L mice. Additionally, Sapanisertib (INK-128) leads to a 50% reduction in prostatic intraepithelial neoplasia (PIN) lesions in PtenL/L mice and triggers programmed cell death across various cancer cell lines in mice^[2].
体外研究	Sapanisertib (INK-128) demonstrates enzymatic inhibitory activity against mTOR with over 100-fold selectivity compared to PI3K kinases^[1]. Sapanisertib (INK-128) selectively reduces the protein levels of YB1, MTA1, vimentin, and CD44 without affecting their mRNA levels in PC3 cells. It also diminishes the invasive capabilities of PC3 prostate cancer cells. Additionally, Sapanisertib (INK-128) impedes cancer cell migration beginning at 6 hours post-treatment, coinciding with the evident reduction in pro-invasion gene expression, and before any alterations in the cell cycle or overall global protein synthesis are observed^[2].

Sapanisertib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
MIA PaCa-2	1-100 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	24971544
PANC-1	1-100 nM	Cell Viability Assay	72 h	inhibits cell viability dose dependently	24971544
PANC-1	50 nM	Cell Viability Assay	24-96 h	inhibits cell viability time dependently	24971544
PANC-1	10-100 nM	Apoptosis Assay	72 h	induces apoptosis dose dependently	24971544

Sapanisertib 动物研究

Dose	Nude Mice: 1 mg/kg - 3 mg/kg^[3] (p.o.), 0.5 mg/kg - 7 mg/kg^[4] (i.p.), 0.3 mg/kg^[5] (i.p.)
Administration	p.o., i.p.

Sapanisertib 参考文献

[1]Liu A, et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009, 6(2), 47-55.

[2]Hsieh AC, et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61.

Sapanisertib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.23mL

0.65mL

0.32mL

16.16mL

3.23mL

1.62mL

32.33mL

6.47mL

3.23mL

Sapanisertib 技术信息

CAS号	1224844-38-5
分子式	C₁₅H₁₅N₇O
分子量	309.326

别名	INK-128;TAK-228;MLN0128
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 55 mg/mL(177.81 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+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 71 mg/mL suspension

沙帕色替 /Sapanisertib {[allProObj[0].p_purity_real_show]}

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Sapanisertib 参考文献

Sapanisertib 实验方案

Sapanisertib 技术信息

最近浏览的产品

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