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.
For research use only. We do not sell to patients.
- CAS No.: 1884341-01-8
- Formula: C28H33N3O3
- Molecular Weight:459.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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.
Chemical Information
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CAS No. 1884341-01-8
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Molecular Weight 459.58
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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