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Cat. No.: HY-110144

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TC-E 5008

TC-E 5008 is a potent mutant IDH1 inhibitor with K_i 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 K_i value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines.

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CAS No.: 50405-58-8
화학식: C₁₃H₁₃NO₂
분자량:215.25

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

TC-E 5008 Chemical Structure

CAS No.: 50405-58-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

R132H IDH1

190 nM (Ki)

R132C IDH1

120 nM (Ki)

WT IDH1

12.3 μM (Ki)

All Isocitrate Dehydrogenase (IDH) Isoforms :

IDH1
IDH2

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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	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]
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]

In Vitro

TC-E 5008 (compound 2; 48 h) inhibits the production of D2HG with an EC₅₀ value of 2.4 μM in HT1080 fibrosarcoma cells , which harbor an IDH1(R132C) mutation^[1].
TC-E 5008 (2-10 μM; 72 h) has anti-proliferative activity on multiple ER positive breast cancer cell lines^[2].

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

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.

Chemical Information

CAS No. 50405-58-8
분자량 215.25
화학식 C₁₃H₁₃NO₂
SMILES

ON1C(CC2=CC=CC=C2)=CC(C)=CC1=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Baisong Zheng, et al. Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase. ACS Med Chem Lett. 2013 Jun 13;4(6):542-546. [Content Brief]

[2]. Vasanth S. Murali, et al. Cancer drug discovery as a low rank tensor completion problem. bioRxiv, March 9, 2021.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
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TC-E 5008

All Isocitrate Dehydrogenase (IDH) Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

TC-E 5008 Related Classifications

HY-110144 Related Classifications