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Gimatecan

Catalog No. T21319 CAS 292618-32-7

Synonyms: LBQ707, STI481

Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.

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Gimatecan, CAS 292618-32-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
5 mg	In stock	$ 288.00
10 mg	In stock	$ 478.00
25 mg	In stock	$ 789.00
50 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 318.00

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Purity: 98.47%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
In vitro	Gimatecan (3 to 300 ng/mL) significantly inhibits the growth of human bladder cancer models (HT1376 and MCR), thus reflecting antiproliferative potency. 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].
In vivo	Gimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth[1].

Synonyms	LBQ707, STI481
Molecular Weight	447.48
Formula	C25H25N3O5
CAS No.	292618-32-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31.5 mg/mL (70.4 mM), when pH is adjusted to 10 with NaOH. Sonication and heating to 60℃ are recommended.

H2O: Insoluble

References and Literature

1. Paola Ulivi, et al. Cellular Basis of Antiproliferative and Antitumor Activity of the Novel Camptothecin Derivative, Gimatecan, in Bladder Carcinoma Models. Neoplasia. 2005 Feb;7(2):152-61. 2. Frapolli R, Zucchetti M, Sessa C, Marsoni S, ViganÃ² L, Locatelli A, Rulli E, Compagnoni A, Bello E, Pisano C, Carminati P, D'Incalci M. Clinical pharmacokinetics of the new oral camptothecin gimatecan: the inter-patient variability is related to alpha1-acid glycoprotein plasma levels. Eur J Cancer. 2010 Feb;46(3):505-16. Epub 2009 Dec 16. PubMed PMID: 20007015. 3. Pecorelli S, Ray-Coquard I, Tredan O, Colombo N, Parma G, Tisi G, KatsarÃ²s D, LhommÃ© C, Lissoni AA, Vermorken JB, du Bois A, Poveda A, Frigerio L, Barbieri P, Carminati P, Brienza S, Guastalla JP. Phase II of oral gimatecan in patients with recurrent epithelial ovarian, fallopian tube or peritoneal cancer, previously treated with platinum and taxanes. Ann Oncol. 2010 Apr;21(4):759-65. Epub 2009 Nov 11. PubMed PMID: 19906760; PubMed Central PMCID: PMC2844948. 4. Pace S, Capocasa F, Tallarico C, Frapolli R, Zucchetti M, Longo A. Determination of total and lactone form of a new camptothecin derivative gimatecan (ST1481) and its metabolite ST1698 in human plasma by high-performance liquid chromatography with fluorimetric detection. J Pharm Biomed Anal. 2009 Oct 15;50(3):507-14. Epub 2009 May 27. PubMed PMID: 19553057.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Lung Cancer Compound Library Anti-Cancer Compound Library DNA Damage & Repair Compound Library Clinical Compound Library Bioactive Compounds Library Max

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Topoisomerase IV inhibitor 1 Levofloxacin Karenitecin 9-Chloromethyl-10-hydroxy-11-F-Camptothecin Pazufloxacin Mesylate Pefloxacin Mesylate Dihydrate Daniquidone Voreloxin

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Keywords

Gimatecan 292618-32-7 DNA Damage/DNA Repair Topoisomerase LBQ707 STI-481 STI 481 LBQ-707 STI481 LBQ 707 inhibitor inhibit

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