![]() Gimatecan structure
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Common Name | Gimatecan | ||
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CAS Number | 292618-32-7 | Molecular Weight | 447.483 | |
Density | 1.4±0.1 g/cm3 | Boiling Point | 780.6±70.0 °C at 760 mmHg | |
Molecular Formula | C25H25N3O5 | Melting Point | N/A | |
MSDS | N/A | Flash Point | 425.9±35.7 °C |
Use of GimatecanGimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1]. |
Name | 7-[(E)-tert-butyloxyiminomethyl]-camptothecin |
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Synonym | More Synonyms |
Description | Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1]. |
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Related Catalog | |
Target |
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]. 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]. 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. |
References |
Density | 1.4±0.1 g/cm3 |
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Boiling Point | 780.6±70.0 °C at 760 mmHg |
Molecular Formula | C25H25N3O5 |
Molecular Weight | 447.483 |
Flash Point | 425.9±35.7 °C |
Exact Mass | 447.179413 |
PSA | 103.01000 |
LogP | 3.42 |
Vapour Pressure | 0.0±2.8 mmHg at 25°C |
Index of Refraction | 1.667 |
Hazard Codes | T+ |
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Precursor 2 | |
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DownStream 0 |
trans-1-Hydroxy-7-phenyl-hepten-(2)-diin-(4,6) |
7-Phenyl-hept-2t-en-4,6-diin-1-ol |
7-tert-butoxyiminomethylcamptothecin |
(E)-7-phenyl-2-hepten-4,6-diyn-1-ol |
7-phenyl-hept-2t-ene-4,6-diyn-1-ol |
ST-1481 |
1-Phenyl-hepten-(5)-trans-diin-(1.3)-ol-(7) |
trans-7-Phenyl-hepten-(2)-diin-(4.6)-ol-(1) |
2-Heptene-4,6-diyn-1-ol,7-phenyl-,(E) |
(4S)-11-[(E)-(tert-butoxyimino)methyl]-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione |
7-(t-butoxy)iminomethylcamptothecin |
1H-Pyrano(3',4':6,7)indolizino(1,2-b)quinoline-11-carboxaldehyde, 4-ethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-, 11-(O-(1,1-dimethylethyl)oxime), (4S)- |
(E)-7-tert-butoxyiminomethyl-camptothecin |
7-hydroxy-1-phenyl-hept-5E-ene-1,3-diyne |
(4S)-4-Ethyl-4-hydroxy-11-[(E)-{[(2-methyl-2-propanyl)oxy]imino}methyl]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione |
1H-Pyrano[3',4':6,7]indolizino[1,2-b]quinoline-11-carboxaldehyde, 4-ethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-, 11-[O-(1,1-dimethylethyl)oxime], (4S)- |
Gimatecan |