Sapanisertib (MLN0128)

目录号:S2811 别名: INK 128,TAK-228

仅限科研使用

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

CAS: 1224844-38-5

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 7924.38 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Sapanisertib (MLN0128)发表文献101篇:

产品安全说明书

mTOR抑制剂选择性比较

相关mTOR产品

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

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  NVvEZYhPTnWwY4Tpc44hSXO|YYm= MVKxNEBvVQ>? MYO3NkBp MkS1bY5kemWjc3XzJIdmdWOrdHHibY5mKHOnboPpeIl3cXS7 MoG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{G1OFQoRjJ2OUexOVQ1RC:jPh?=
PANC-1  MY\GeY5kfGmxbjDBd5NigQ>? NWHaVHdqPTBibl2= M1z0PVQ5KGh? M2O0XIRqe3K3cITzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25? MoDsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{G1OFQoRjJ2OUexOVQ1RC:jPh?=
PANC-1  MVzGeY5kfGmxbjDBd5NigQ>? NH\jSZoyOC93MDDuUS=> M{nyRlI1KGh? NIq5PWZlemGvYYTpZ4FtdHliaX7obYJqfHNicHjvd5Bpd3K7bHH0bY9vKG:oIETFMWJROS2VNluxJEhuXE:UQ{GgZYN1cX[jdHnvckBqdmSrY3H0c5J{MSCjbnSgRYt1KGG2IGPldkA1PzNiKITo[UBuXE:UQ{KgZYN1cX[jdHnvckBqdmSrY3H0c5Iq NIHkOYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEm3NVU1PCd-MkS5O|E2PDR:L3G+
PANC-1  NGnoTldCeG:ydH;zbZMhSXO|YYm= NFK0[WoyOC1zMECgcm0> NH\Jd2Y4OiCq NIr4NpdqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 NY\FbpJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|E2PDRpPkK0PVcyPTR2PD;hQi=>
MIA PaCa-2 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2PzUFEuOTByIH7N NWCzemNrPzJiaB?= NVXLOYV4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5MUW0OEc,OjR7N{G1OFQ9N2F-
PANC-1  NWnQWWlmS2WubDDWbYFjcWyrdImgRZN{[Xl? NETSZow2OCCwTR?= MXyyOE06PiCq M1nOOolvcGmkaYTzJINmdGxidnnhZoltcXS7IITpcYUh\GWyZX7k[Y51dHl? NYTVUWJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|E2PDRpPkK0PVcyPTR2PD;hQi=>
PANC-1  NXH0VVVxS2WubDDWbYFjcWyrdImgRZN{[Xl? NELyU44yNTFyMDDuUS=> MnHCO|IhcA>? MX3pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NYTOVZNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O|E2PDRpPkK0PVcyPTR2PD;hQi=>
TC32 MVrxTHRUKGG|c3H5 MkTVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? NVrhSm5wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
U-2 OS NHTzd2xyUFSVIHHzd4F6 M4DmZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCXLUKgU3Mh[2WubIO= NULKdVhxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NVPBbIVYeUiWUzDhd5NigQ>? MofJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? NYfaOm5uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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BT-12 NYqx[5N2eUiWUzDhd5NigQ>? MnvjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| NGjlfJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) MUDxTHRUKGG|c3H5 NXPxeVdpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz M{jLOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 NUTtRnhweUiWUzDhd5NigQ>? NXTOeI1leUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NEXPVJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 MV7xTHRUKGG|c3H5 M3Pn[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= Mke4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NFm1elVyUFSVIHHzd4F6 NG\XXohyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBNSU5vNTDj[Yxtew>? MmiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY MnzRdWhVWyCjc4PhfS=> NIHUUXhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBFSU:\IHPlcIx{ NEfB[Wo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NUPpNGN[eUiWUzDhd5NigQ>? MoDTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? NGT1OVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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A673 MmHHdWhVWyCjc4PhfS=> M1nC[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq NYPae4RKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 M2f4WJFJXFNiYYPzZZk> M3\RW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ NYTuOVlbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30 MULxTHRUKGG|c3H5 Mof1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? M4LTflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M{fOeZFJXFNiYYPzZZk> NVfLd3R6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NWPvUI5jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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U-2 OS NFjoUo5yUFSVIHHzd4F6 NXnWeXc2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy| MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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Assay
Methods Test Index PMID
Western blot FKBP1 / MARS / CDC25A / TCL1A p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6 c-Jun CD44 / Vimentin p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt 25849580 27462815 29899840 25425103
Growth inhibition assay Cell viability 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

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04250545 Suspended 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) November 9 2020 Phase 1
NCT02575339 Terminated Drug: MLN0128|Drug: MLN0128 (RP2D)|Drug: Sorafenib Hepatocellular Carcinoma|Liver Cancer|HCC Kathy Miller|Millennium Pharmaceuticals Inc.|Big Ten Cancer Research Consortium July 18 2016 Phase 1|Phase 2
NCT02719691 Completed Drug: Alisertib|Drug: MLN0128 Metastatic Breast Cancer|Solid Tumors University of Colorado Denver May 13 2016 Phase 1
NCT02514824 Completed Drug: MLN0128 Merkel Cell Carcinoma Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. October 2015 Phase 1|Phase 2
NCT02244463 Active not recruiting Drug: MLN0128 Anaplastic Thyroid Cancer|Thyroid Cancer Dana-Farber Cancer Institute|Millennium Pharmaceuticals Inc. July 2015 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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.

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