MCT1-IN-3
Based on 1 Customer Validation
MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.65%
- CAS 番号: 2878360-80-4
- 分子式: C22H19N3O4
- 分子量:389.40
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
IC50: 81.0 nM (MCT1)[1]
GI50: 20 μM (A-549); 15.1 μM (MCF-7)[1]
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 ADR | EC50 |
0.793 μM
Compound: 24
|
Reversal of multi-drug resistance in human A2780 ADR cells expressing ABCB1 incubated for 72 hrs by MTT assay
Reversal of multi-drug resistance in human A2780 ADR cells expressing ABCB1 incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A2780 ADR | GI50 |
110 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 3.5 uM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 3.5 uM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A2780 ADR | GI50 |
214 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 2 uM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 2 uM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A2780 ADR | GI50 |
32.2 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 5 uM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 5 uM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A2780 ADR | GI50 |
332 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 1 uM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A2780 ADR cells expressing ABCB1 assessed as doxorubicin at 1 uM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A549 | GI50 |
19.4 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin IC50 at 500 nM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin IC50 at 500 nM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A549 | GI50 |
20 μM
Compound: 24
|
Antiproliferative activity against human A549 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A549 | GI50 |
27.7 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 100 nM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 100 nM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| A549 | GI50 |
40 nM
Compound: 24
|
Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 50 nM incubated for 72 hrs by MTT assay
Induction of doxorubicin sensitization in human A549 cells expressing MCT1 assessed as doxorubicin GI50 at 50 nM incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
| MCF7 | GI50 |
15.1 μM
Compound: 24
|
Antiproliferative activity against human MCF7 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
|
[PMID: 36584238] |
MCT1-IN-3 (compound 24) has inhibitory activity for MCT1 with an IC50 value of 81.0 nM[1].
MCT1-IN-3 has great antiproliferative activities against the MCT1-expressing cancer cell lines A-549 and MCF-7 with GI50 values of 20 μM and 15.1 μM, respectively[1].
MCT1-IN-3 (5 μM; 24 h) leads to cancer cell cycle arrest as well as apoptosis[1].
MCT1-IN-3 (1.0, 2.0, 3.5, and 5.0 μM) shows to sensitize these cancer cells toward an antineoplastic agent[1].
MCT1-IN-3 has also significant inhibitory power against the multidrug transporter ABCB1 and shows to reverse ABCB1-mediated multidrug resistance (MDR) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A-549 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Caused a disruption of the cell cycle of A-549 cancer cells, indicated by a shift from the predominant Go/G, phase.
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Cell Line:A-549 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Increased the percentage of total apoptotic cells by a factor of 13 from 0.51 to 6.68%.
化学情報
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CAS 番号 2878360-80-4
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性状 Solid
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分子量 389.40
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分子式 C22H19N3O4
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Color Off-white to light yellow
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SMILES
COC(/C(C#N)=C/C1=CN(C2=CC=CC=C12)CC(NC3=CC=C(C=C3)OC)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
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- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)