Sapanisertib (MLN0128)

For research use only. Not for use in humans.

目录号:S2811 别名: INK 128,TAK-228

Sapanisertib (MLN0128) Chemical Structure

CAS No. 1224844-38-5

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1810.73 现货
RMB 1405.88 现货
RMB 2189.56 现货
RMB 7924.38 现货
RMB 10401.3 现货
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客户使用Selleck生产的Sapanisertib (MLN0128)发表文献67篇:

产品安全说明书

mTOR抑制剂选择性比较

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)
1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM 230 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC-1  M1e2WWNmdGxiVnnhZoltcXS7IFHzd4F6 MXWxMVExOCCwTR?= MV63NkBp NVPVdHN{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVnyWWNqOjR7N{G1OFQ>
PANC-1  M1HwT2NmdGxiVnnhZoltcXS7IFHzd4F6 M{f5V|UxKG6P MmrBNlQuQTZiaB?= MofUbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHlidHnt[UBl\XCnbnTlcpRtgQ>? MWqyOFk4OTV2NB?=
MIA PaCa-2 M2LuTGNmdGxiVnnhZoltcXS7IFHzd4F6 NXnkdGV6OS1zMECgcm0> NWfSV3dIPzJiaB?= M1H2[4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NYDaTmVCOjR7N{G1OFQ>
PANC-1  M2W5VGFxd3C2b4Ppd{BCe3OjeR?= NHvwV5UyOC1zMECgcm0> NFjN[2M4OiCq MXjpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 Mm\ZNlQ6PzF3NES=
PANC-1  NEHsSoNHfW6ldHnvckBCe3OjeR?= MkD2NVAwPTBibl2= NXz2UGN3OjRiaB?= Ml3r[JJidWG2aXPhcIx6KGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iB2RT3CVFEuWz[NMTCocXRQWkNzIHHjeIl3[XSrb36gbY5lcWOjdH;yd{kh[W6mIFHreEBifCCVZYKgOFc{KCi2aHWgcXRQWkN{IHHjeIl3[XSrb36gbY5lcWOjdH;yLS=> NWK3S25{OjR7N{G1OFQ>
PANC-1  NGe4VFNHfW6ldHnvckBCe3OjeR?= MlOyOVAhdk1? NITEXng1QCCq NXzvbop[\Gm|coXweJMh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?= NFHWZ5ozPDl5MUW0OC=>
PANC-1  M3PUWGZ2dmO2aX;uJGF{e2G7 NITuXW4yOCCwTR?= MYi3NkBp NX3oS3g{cW6lcnXhd4V{KGenbXPpeIFjcW6nIIPlcpNqfGm4aYT5 M3qwNFI1QTdzNUS0

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt; 

PubMed: 25425103     


INK128 inhibits mTOR signaling in neuroblastoma cells. A panel of six neuroblastoma cell lines was treated with 0.2 μM INK128 for 0 hr, 4 hrs, and 6 hrs, lysed, subjected to SDS-PAGE and immunoblotted with indicated antibodies. β-Actin was detected as a l䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ

CD44 / Vimentin; 

PubMed: 29899840     


CD44 (high) SNU423 cells were treated with increasing concentrations of INK128 for 48 h. CD44, vimentin and downstream effectors of mTOR pathway were evaluated by immunoblotting. 

c-Jun; 

PubMed: 27462815     


Representative western blot of 293T cells after 24 h treatment with INK128. The results are representative of three independent experiments. 

p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6; 

PubMed: 25849580     


SUDHL-2 and SUDHL-4 cells were treated with either EtOH for 24 h, INK128 for 3 h at the concentrations as indicated, or 20 nM rapamycin (Rap.) for 3 h. Cell lysates were analyzed by western blotting for phosphorylation states and total levels of indicated䲧疝Ỵ疞㧀疜

FKBP1 / MARS / CDC25A / TCL1A; 

PubMed: 25849580     


SUDHL-2 and SUDHL-4 cells are treated with EtOH (20 mM) for 48 h or INK128 (40 nM) for 24 h. Protein levels of validated genes were analyzed by western blotting.

25425103 29899840 27462815 25849580
Growth inhibition assay
Cell viability ; 

PubMed: 25425103     


Six neuroblastoma cell lines were treated with the indicated concentrations of INK128 for 48 hrs. Cell viability was then measured by adding the mixture of 10 μL of CCK-8 and 190 μL of RPMI 1640 and reading the absorbance at 450 nm. Data were represented 䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ

25425103
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 62 mg/mL (200.43 mM)
Ethanol 2 mg/mL (6.46 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 309.33
化学式

C15H15N7O

CAS号 1224844-38-5
储存条件 粉状
溶于溶剂
别名 INK 128,TAK-228

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04250545 Recruiting Drug: Sapanisertib|Drug: Telaglenastat Hydrochloride 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) June 12 2020 Phase 1
NCT02575339 Active not recruiting Drug: MLN0128|Drug: MLN0128 (RP2D)|Drug: Sorafenib Hepatocellular Carcinoma|Liver Cancer|HCC Bert O''Neil MD|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium July 2016 Phase 1|Phase 2
NCT02719691 Recruiting Drug: Alisertib|Drug: MLN0128 Metastatic Breast Cancer|Solid Tumors University of Colorado Denver May 13 2016 Phase 1
NCT02244463 Recruiting Drug: MLN0128 Anaplastic Thyroid Cancer|Thyroid Cancer Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. July 2015 Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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.

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID