TAK-733

For research use only. Not for use in humans.

目录号:S2617

TAK-733 Chemical Structure

CAS No. 1035555-63-5

TAK-733是一种有效的,选择性的MEK变构抑制剂,作用于MEK1,IC50为3.2 nM,抑制Abl1, AKT3, c-RAF, CamK1, CDK2及c-Met等活性。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2764.51 现货
RMB 1402.58 现货
RMB 2613.75 现货
RMB 7932.61 现货
RMB 20229.3 现货
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客户使用Selleck生产的TAK-733发表文献17篇:

客户使用该产品的5个实验数据:

  • Effect of MEK inhibitor TAK-733 in A549 cells. A549 cells were incubated with increasing concentrations of TAK-733 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

    Dr.Wang from Southern Medical Hospital . TAK-733 purchased from Selleck.

  • Mouse carcinoma cells were treated with the inhibitors for 16 and 40 h at the concentrations indicated. The effect on S-phase was evident at 16 hrs. (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10nM, GSK1120212=<1nM.

    Jonas Nilsson, PhD from University of Gothenburg. TAK-733 purchased from Selleck.

  • After starved in serum-free medium for 24 h, T47D cells incubated with the indicated concentrations of TAK-733 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. TAK-733 purchased from Selleck.

  • (c) Fold induction of apoptotic cells after 3-day compound or vehicle (DMSO) treatment, as measured by annexin V positivity. Error bars indicate s.d.'s (n=4). **P<0.01, ***P<0.001, two-way ANOVA with Holm Sidak multiple comparisons correction.

    Nat Commun, 2016, 7:13701.. TAK-733 purchased from Selleck.

  • Both PI3K/Akt and MAPK signaling pathways are essential in lung cancer cells harboring wild-type EGFR (A) PI3K inhibition suppressed proliferation of lung cancer cells harboring mutant or wild-type EGFR. A549 and PC-9 cells were incubated in the presence of various concentrations of GSK2126458 or PF04691502. Cell extracts were prepared after 1 h of treatment and immunoblotted with the indicated antibodies (upper panel). Cell growth was measured by MTT assay after 72 h (lower panel). (B) MEK inhibition suppressed proliferation of lung cancer cells harboring mutant or wild-type EGFR. A549 and PC-9 cells were incubated in the presence of various concentrations of AZD-8330 or TAK-733. Cell extracts were prepared after 1 h of treatment and immunoblotted with the indicated antibodies (upper panel). Cell growth was measured by MTT assay after 72 h (lower panel).

    Oncotarget, 2016, 7(13):16273-81.. TAK-733 purchased from Selleck.

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 TAK-733是一种有效的,选择性的MEK变构抑制剂,作用于MEK1,IC50为3.2 nM,抑制Abl1, AKT3, c-RAF, CamK1, CDK2及c-Met等活性。Phase 1。
靶点
MEK1 [1]
(Cell-free assay)
3.2 nM
体外研究

TAK-733是高度有效的选择性MEK变构位点抑制剂,IC50 为3.2 nM。TAK-733表现出有效的酶和细胞活性,对细胞中ERK磷酸化作用的EC50为1.9 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COLO205 NH;ye3ZEgXSxdH;4bYNqfHliYYPzZZk> MYG3NkBpenN? NX;XS4VWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0:OT{KwOUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDFR|UxRTBwMECyNe69VS5? MnX6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|MUC2NVMoRjJzM{GwOlE{RC:jPh?=
A375 Mo\RR5l1d3SxeHnjbZR6KGG|c3H5 M4TFZlczKGi{cx?= NVKxSGkzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTN5NTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCHQ{WwQVAvODB|Md88UU4> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTNzME[xN{c,OjF|MUC2NVM9N2F-
COLO205 M1XFZmZ2dmO2aX;uJIF{e2G7 M321ZWlvcGmkaYTpc44hd2ZiTVXLNUBqdiCqdX3hckBEV0yRMkC1JINmdGy|LDDJR|UxRTBwMEC2PVLPxE1w NVK4[pkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OVU1OjZpPkK0O|U2PDJ4PD;hQi=>
DAOY MkjxdWhVWyCjc4PhfS=> NILHSVhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NGXRSWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
U-2 OS MWfxTHRUKGG|c3H5 M{XFV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCXLUKgU3Mh[2WubIO= M1[wTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NVLYZokzeUiWUzDhd5NigQ>? M1HC[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz NWjWbYZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NUHDTYxyeUiWUzDhd5NigQ>? M3rNeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| NFywbnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD MYjxTHRUKGG|c3H5 NF3JTWNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pRb / Cyclin E ; 

PubMed: 26918363     


The effect of treatment for 48 h on cell cycle signaling pRb and Cyclin E in H929 cells by Western blotting

p-ERK / p-AKT / p-S6R / p-GSK3 ; 

PubMed: 26918363     


Effect of TAK-733 (0, 2 μM) for 48 h on proliferation signaling of pERK, pAKT, pS6R and pGSK3 in H929 cells by Western blotting. 

26918363
Growth inhibition assay
Cell viability; 

PubMed: 26918363     


The effect of TAK-733, MEK inhibitor (0-25 μM) on proliferation of MM.1S, U266, H929, RPMI-8826 and OPM2 cells.

26918363
体内研究 TAK-733在人体肿瘤,包括黑色素瘤,结肠直肠癌,NSCLC,胰腺癌和乳腺癌的小鼠异种移植物模型中表现出广谱抗肿瘤活性。TAK-733具有良好的药代动力学和药效动力学耐受性,对于人类可每天一次口服给药。[1] TAK-733的最大有效剂量为10 mg/kg,每天一次。[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)

动物实验:[2]
- 合并
  • Animal Models: 负荷人实体瘤异种移植物,包括 NSCLC (NCI H23 [KRAS 和 LKB1 突变]),CRC (SW620 [KRAS,APC,p53 突变])以及胰腺癌(Panc 1 和 Capan 1 [KRAS 突变型] 和 BxPC-3 [无 MAPK 突变])的免疫功能缺陷小鼠模型。
  • Dosages: 10 mg/kg
  • Administration: 口服给药,每天一次,持续21天
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 101 mg/mL (200.3 mM)
Water Insoluble
Ethanol Insoluble

* 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 504.23
化学式

C17H15F2IN4O4

CAS号 1035555-63-5
储存条件 粉状
溶于溶剂
别名 N/A

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、SDS / 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、SDS / 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
NCT01613261 Withdrawn Drug: TAK-733 and alisertib Advanced Nonhematologic Malignancies Millennium Pharmaceuticals Inc. August 2013 Phase 1
NCT00948467 Completed Drug: TAK-733 Advanced Non-hematologic Malignancies|Advanced Metastatic Melanoma Millennium Pharmaceuticals Inc. December 2009 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID