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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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CAS No.: 1884341-01-8
Formule: C₂₈H₃₃N₃O₃
Masse moléculaire:459.58

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

Data Sheet (272 KB)

Telomerase-IN-8 Chemical Structure

CAS No.: 1884341-01-8

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
Bcap37	IC₅₀	3.37 μM Compound: 13i	Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay	[PMID: 26900656]
GES1	IC₅₀	1.64 mM Compound: 13i	Cytotoxicity against human GES-1 cells after 48 hrs by MTT assay Cytotoxicity against human GES-1 cells after 48 hrs by MTT assay	[PMID: 26900656]
HepG2	IC₅₀	2.45 μM Compound: 13i	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 26900656]
L02	IC₅₀	1.62 mM Compound: 13i	Cytotoxicity against human L02 cells after 48 hrs by MTT assay Cytotoxicity against human L02 cells after 48 hrs by MTT assay	[PMID: 26900656]
MGC-803	IC₅₀	0.98 μM Compound: 13i	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	[PMID: 26900656]
MGC-803	IC₅₀	2.96 μM Compound: 13i	Cytotoxicity against human MGC803 cells after 48 hrs by MTT assay Cytotoxicity against human MGC803 cells after 48 hrs by MTT assay	[PMID: 26900656]
PC-3	IC₅₀	4.87 μM Compound: 13i	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 26900656]

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.

Chemical Information

CAS No. 1884341-01-8
Masse moléculaire 459.58
Formule C₂₈H₃₃N₃O₃
SMILES

O=C1OC2=C(C=C1C3=NN(C(C3)C4=CC=CC=C4)C(CN(CCCC)CCCC)=O)C=CC=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 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)
Instruction de manipulation (2659 KB)

Références

[1]. Wang Y, et al. Dihydropyrazole derivatives as telomerase inhibitors: Structure-based design, synthesis, SAR and anticancer evaluation in vitro and in vivo. Eur J Med Chem. 2016 Apr 13;112:231-251. [Content Brief]

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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.

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100 mg

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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