Sapanisertib (MLN0128)

别名: INK 128,TAK-228

Sapanisertib (MLN0128, INK 128, TAK-228) 是一种有效的,选择性mTOR抑制剂,在无细胞试验中IC50为1 nM;对I型PI3K亚型的作用效果低200倍以上,与Rapamycin相比,优先抑制mTORC1/2,且对促侵袭基因敏感。Phase 1。

Sapanisertib (MLN0128) Chemical Structure

Sapanisertib (MLN0128) Chemical Structure

CAS: 1224844-38-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1810.73 现货
5mg 1405.88 现货
50mg 7924.38 现货
100mg 10401.3 现货
1g 32678.1 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

Sapanisertib (MLN0128)相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
U87 Function assay Inhibition of mTOR in human U87 cells assessed as reduction in pRAS40 phosphorylation by Western blot method ChEMBL
U87 Function assay Inhibition of mTOR pS6K in human U87 cells assessed as inhibition of 4EBP1 phosphorylation by Western blot analysis ChEMBL
PANC-1  Function Assay 50 nM 48 h disrupts cell cycle progression 24971544
PANC-1  Function Assay 10 nM 72 h increases LY 188011 sensitivity 24971544
PANC-1  Function Assay 10/50 nM 24 h dramatically inhibits phosphorylation of 4E-BP1-S6K1 (mTORC1 activation indicators) and Akt at Ser 473 (the mTORC2 activation indicator) 24971544
PANC-1  Apoptosis Assay 10-100 nM 72 h induces apoptosis dose dependently 24971544
MIA PaCa-2 Cell Viability Assay 1-100 nM 72 h inhibits cell viability dose dependently 24971544
PANC-1  Cell Viability Assay 50 nM 24-96 h inhibits cell viability time dependently 24971544
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
A2058 Function assay 1 hr Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in 4E-BP1 phosphorylation after 1 hr by Western blot analysis 30359003
SKOV3 Function assay 1 hr Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis 30359003
SKOV3 Function assay 1 hr Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6K phosphorylation after 1 hr by Western blot analysis 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in S6K phosphorylation after 1 hr by Western blot analysis 30359003
SKOV3 Function assay 1 hr Inhibition of TORC2 in human SKOV3 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis 30359003
U87 Function assay Inhibition of mTOR in human U87 cells assessed as reduction in pAKT phosphorylation at residue 47 by Western blot method ChEMBL
PANC-1  Cell Viability Assay 1-100 nM 72 h inhibits cell viability dose dependently 24971544
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
SKOV3 Function assay 1 hr Inhibition of TORC1 in human SKOV3 cells assessed as decrease in 4E-BP1 phosphorylation after 1 hr by Western blot analysis 30359003
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells measured after 72 hrs by Alamar blue dye-based fluorescence analysis, EC50 = 0.1 μM. ChEMBL
U87 Function assay Inhibition of mTOR in human U87 cells assessed as reduction in p4EBP1 phosphorylation by Western blot method ChEMBL
U87 Function assay Inhibition of mTOR pS6K in human U87 cells assessed as inhibition of RAS40 phosphorylation by Western blot analysis ChEMBL
U87 Antitumor assay 0.3 to 3 mg/kg 14 days Antitumor activity against human U87 cells xenografted in mouse assessed as tumor growth inhibition at 0.3 to 3 mg/kg measured after 14 days ChEMBL
点击查看更多细胞系数据

生物活性

产品描述 Sapanisertib (MLN0128, INK 128, TAK-228) 是一种有效的,选择性mTOR抑制剂,在无细胞试验中IC50为1 nM;对I型PI3K亚型的作用效果低200倍以上,与Rapamycin相比,优先抑制mTORC1/2,且对促侵袭基因敏感。Phase 1。
靶点
mTOR [3]
(Cell-free assay)
mTOR [3]
(Cell-free assay)
PI3Kα [3]
(Cell-free assay)
PI3Kγ [3]
(Cell-free assay)
PI3Kδ [3]
(Cell-free assay)
点击更多
1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM 230 nM
体外研究(In Vitro)
体外研究活性

INK 128 表现对mTOR酶的抑制活性并对PI3K激酶的选择性超过100倍。[1]

作为TORC1/2抑制剂,INK 128抑制TORC1的下游底物S6和4EBP1的磷酸化。此外,INK 128也显示了对雷帕霉素和泛PI3K抑制剂耐受的细胞株的有效抑制效应。[2]

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt CD44 / Vimentin c-Jun p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6 FKBP1 / MARS / CDC25A / TCL1A 25425103
Growth inhibition assay Cell viability 25425103
体内研究(In Vivo)
体内研究活性

在ZR-75-1乳腺癌异种移植模型中,INK 128(0.3 mg/kg/day)的处理表现了肿瘤生长抑制效果。[1]

在多种移植体模型中,每日口服给药INK 128抑制血管生成和肿瘤生长。[2]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04250545 Recruiting
Leptomeningeal Neoplasm|Metastatic Lung Non-Small Cell Carcinoma|Metastatic Malignant Neoplasm in the Brain|Recurrent Lung Non-Small Cell Carcinoma|Stage IV Lung Cancer AJCC v8|Stage IVA Lung Cancer AJCC v8|Stage IVB Lung Cancer AJCC v8
National Cancer Institute (NCI)
October 26 2020 Phase 1
NCT02575339 Terminated
Hepatocellular Carcinoma|Liver Cancer|HCC
Kathy Miller|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium
July 18 2016 Phase 1|Phase 2
NCT02719691 Completed
Metastatic Breast Cancer|Solid Tumors
University of Colorado Denver
May 13 2016 Phase 1
NCT02514824 Completed
Merkel Cell Carcinoma
Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc.
October 2015 Phase 1|Phase 2

化学信息&溶解度

分子量 309.33 分子式

C15H15N7O

CAS号 1224844-38-5 SDF Download Sapanisertib (MLN0128) SDF
Smiles CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 62 mg/mL ( (200.43 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 2 mg/mL (6.46 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们

常见问题及建议解决方法

问题 1:
What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?

回答:
You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.

Tags: buy Sapanisertib (MLN0128) | Sapanisertib (MLN0128) supplier | purchase Sapanisertib (MLN0128) | Sapanisertib (MLN0128) cost | Sapanisertib (MLN0128) manufacturer | order Sapanisertib (MLN0128) | Sapanisertib (MLN0128) distributor
在线咨询
联系我们