Telomerase-IN-8
Telomerase-IN-8 is an orally active telomerase inhibitor, with an IC50 value of 0.98 μM. Telomerase-IN-8 exhibits potent antiproliferative activity against multiple tumor cell lines, including PC3, Bcap-37, MGC-803 and HepG2. Telomerase-IN-8 demonstrates potent antitumor efficacy in S180 sarcoma or HepG2 hepatoma xenograft mice. Telomerase-IN-8 can be used for the study of telomerase-targeted anticancer.
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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。
- CAS 番号: 1884341-01-8
- 分子式: C28H33N3O3
- 分子量:459.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bcap37 | IC50 |
3.37 μM
Compound: 13i
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Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay
Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay
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[PMID: 26900656] |
| GES1 | IC50 |
1.64 mM
Compound: 13i
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Cytotoxicity against human GES-1 cells after 48 hrs by MTT assay
Cytotoxicity against human GES-1 cells after 48 hrs by MTT assay
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[PMID: 26900656] |
| HepG2 | IC50 |
2.45 μM
Compound: 13i
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Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
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[PMID: 26900656] |
| L02 | IC50 |
1.62 mM
Compound: 13i
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Cytotoxicity against human L02 cells after 48 hrs by MTT assay
Cytotoxicity against human L02 cells after 48 hrs by MTT assay
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[PMID: 26900656] |
| MGC-803 | IC50 |
0.98 μM
Compound: 13i
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Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay
Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay
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[PMID: 26900656] |
| MGC-803 | IC50 |
2.96 μM
Compound: 13i
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Cytotoxicity against human MGC803 cells after 48 hrs by MTT assay
Cytotoxicity against human MGC803 cells after 48 hrs by MTT assay
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[PMID: 26900656] |
| PC-3 | IC50 |
4.87 μM
Compound: 13i
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Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
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[PMID: 26900656] |
Telomerase-IN-8 (Compound 13i) (48 h) shows potent antiproliferative activity against PC3, Bcap-37, MGC-803, and HepG2 tumor cells, with IC50 values of 4.87 μM, 3.37 μM, 2.96 μM, and 2.45 μM, respectively[1].
Telomerase-IN-8 (48 h) exhibits low toxicity to human normal GES-1 and L-02 cells, with IC50 values of 1.64 mM and 1.62 mM, respectively[1].
Telomerase-IN-8 displays potent inhibitory activity against human telomerase modified TRAP assay in MGC-803 cell extracts, with an IC50 value of 0.98 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:S180 sarcoma cells or HepG2 hepatoma cells (2 × 106 cells in 0.2 mL sterile normal saline, prepared from 7-day-old tumor ascites) were subcutaneously implanted into the right front armpit of Kunming mice [1]
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Dosage:60 mg/kg
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Administration:p.o., once daily, 10 consecutive days
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Result:Achieved tumor growth inhibition (TGI) rates of 48.9% and 46.1% in S180 sarcoma-bearing and HepG2 hepatoma-bearing Kunming mice .
Showed no significant changes in body weight.
化学情報
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CAS 番号 1884341-01-8
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分子量 459.58
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分子式 C28H33N3O3
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SMILES
O=C1OC2=C(C=C1C3=NN(C(C3)C4=CC=CC=C4)C(CN(CCCC)CCCC)=O)C=CC=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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