2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. TC-E 5008

TC-E 5008 是一种有效的突变体 IDH1 抑制剂，对 R132H 和 R132C IDH1 突变体的Ki 值分别为 190 nM 和 120 nM。TC-E 5008 对 WT-IDH1 表现出非常弱的活性，Ki 值为 12.3 μM。TC-E 5008 对多种 ER 阳性乳腺癌细胞系具有抗增殖活性。

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TC-E 5008 Chemical Structure

TC-E 5008 Chemical Structure

CAS No. : 50405-58-8

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TC-E 5008 相关抗体

Top Publications Citing Use of Products

查看 Isocitrate Dehydrogenase (IDH) 亚型特异性产品:

查看所有亚型
IDH1 IDH2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines[1][2].

IC50 & Target[1]

R132H IDH1

190 nM (Ki)

R132C IDH1

120 nM (Ki)

WT IDH1

12.3 μM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-1080 IC50
> 30 μM
Compound: 2
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in D2HG production incubated for 48 hrs by HPLC-MS method
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in D2HG production incubated for 48 hrs by HPLC-MS method
[PMID: 25271760]
HT-1080 EC50
2.4 μM
Compound: 2
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as production of D-2-hydroxyglutaric acid formation after 48 hrs by HPLC-MS method
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as production of D-2-hydroxyglutaric acid formation after 48 hrs by HPLC-MS method
[PMID: 23795241]
Vero CC50
> 100 μM
Compound: 6f
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
[PMID: 35635945]
WI-38 EC50
> 50 μM
Compound: 2
Inhibition of cell proliferation of human WI38 cells by CCK8 assay
Inhibition of cell proliferation of human WI38 cells by CCK8 assay
[PMID: 25271760]
WI-38 EC50
> 50 μM
Compound: 2
Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by MTS assay
Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by MTS assay
[PMID: 23795241]
体外研究
(In Vitro)

TC-E 5008 (化合物 2; 48 小时) 抑制具有 IDH1(R132C) 突变的 HT1080 纤维肉瘤细胞中 D2HG 的产生，EC50 值为 2.4 μM[1]。
TC-E 5008 (2-10 μM; 72 小时) 对多种 ER 阳性乳腺癌细胞系具有抗增殖活性[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TC-E 5008 相关抗体:

Cell Proliferation Assay[2]

Cell Line: MCF-7, ZR-75, T-47D, MDA-MB-23 cells
Concentration: 2, 4, 6, 8, 10 μM
Incubation Time: 72 h
Result: Had anti-proliferative activity.
分子量

215.25

Formula

C13H13NO2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TC-E 5008 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TC-E 500850405-58-8Isocitrate Dehydrogenase (IDH)mutant IDH1R132HR132Cbreast cancerInhibitorinhibitorinhibit

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目录号：
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