1. Cell Cycle/DNA Damage
  2. Telomerase
  3. 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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Telomerase-IN-8

Telomerase-IN-8 Chemical Structure

CAS No. : 1884341-01-8

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Description

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[1].

In Vitro

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.

In Vivo

Telomerase-IN-8 (Compound 13i) (60 mg/kg, p.o., once daily, 10 consecutive days) demonstrates potent antitumor efficacy in S180 sarcoma or HepG2 hepatoma xenograft Kunming mice[1].

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

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]
Dosage: 60 mg/kg
Administration: p.o., once daily, 10 consecutive days
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.
Molecular Weight

459.58

Formula

C28H33N3O3

CAS No.
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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Telomerase-IN-8
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HY-204056
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