
Gimatecan
CAS No. 292618-32-7
Gimatecan( —— )
Catalog No. M33718 CAS No. 292618-32-7
Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
Purity : >98% (HPLC)






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2MG | 176 | Get Quote |
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5MG | 274 | Get Quote |
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10MG | 454 | Get Quote |
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25MG | 726 | Get Quote |
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50MG | 994 | Get Quote |
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Biological Information
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Product NameGimatecan
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NoteResearch use only, not for human use.
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Brief DescriptionGimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
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DescriptionGimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
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In VitroGimatecan (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).Cell Proliferation AssayCell 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.
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In VivoGimatecan (2 mg/kg; treatment per os, every fourth day for four times) is effective for inhibiting tumor growth.Animal Model:Athymic Swiss nude mice bearing HT1376 model Dosage:2 mg/kg Administration:Treatment per os, every fourth day for four times Result:Caused a marked tumor growth inhibition during treatment.
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetTopoisomerase
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RecptorTopoisomerase
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Research Area——
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Indication——
Chemical Information
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CAS Number292618-32-7
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Formula Weight447.48
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Molecular FormulaC25H25N3O5
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 33.33 mg/mL (74.48 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C; )
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SMILESCC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccccc4c(\C=N\OC(C)(C)C)c3Cn1c2=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.?
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