1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Gimatecan

Gimatecan (Synonyms: ST1481)

Cat. No.: HY-B0063 Purity: 98.01%
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Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.

For research use only. We do not sell to patients.

Gimatecan Chemical Structure

Gimatecan Chemical Structure

CAS No. : 292618-32-7

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Description

Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1].

IC50 & Target[1]

Topoisomerase I

 

In Vitro

Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency[1].
Gimatecan causes a persistent S-phase arrest At 0.003 µg/mL and the number of S-phase cells increased after treatment with a higher concentration (0.03 µg/mL)[1].

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

Cell Proliferation Assay[1]

Cell Line: HT1376 cells harbor a p53 mutation; MCR cells harbor two p53 mutations: one in exon 4 (CGC→CCC) and one in exon 9 (CAG→TAG)
Concentration: 3 to 300 ng/mL
Incubation Time: 1, 6, and 24 hours
Result: IC50s of 90±3 and 9.0±0.4 ng/mL for MCR and HT1376 cells after treatment for 1 hours.
IC50s of 5.0±0.2 and 2.8±0.1 ng/mL for MCR and HT1376 cells after treatment for 24 hours.
The growth-inhibitory effect was dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells at least following a short-term exposure.
In Vivo

Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth[1].

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

Animal Model: Athymic Swiss nude mice bearing HT1376 model[1]
Dosage: 2 mg/kg
Administration: Treatment per os, every fourth day for four times
Result: Caused a marked tumor growth inhibition during treatment.
Clinical Trial
Molecular Weight

447.48

Formula

C₂₅H₂₅N₃O₅

CAS No.

292618-32-7

SMILES

CC(C)(C)O/N=C/C1=C2C(C(N3C2)=CC([[email protected]@]4(O)CC)=C(COC4=O)C3=O)=NC5=CC=CC=C15

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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Keywords:

GimatecanST1481ST 1481ST-1481TopoisomerasetopoisomerasecamptothecinantitumorbladdercancerInhibitorinhibitorinhibit

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