| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vitro |
Gimatecan exhibits antiproliferative potency as evidenced by its significant growth inhibition of human bladder cancer models (HT1376 and MCR) at concentrations of 3 to 300 ng/mL [1]. After treatment with higher concentrations (0.03 µg/mL), gammatecan produces sustained S-phase arrest at 0.003 µg/mL and increases the number of S-phase cells [1]. Identification of cell proliferation [1]
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| ln Vivo |
Gimatecan (2 mg/kg; four doses taken orally every four days) effectively inhibits the growth of tumors [1].
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| Cell Assay |
Cell proliferation detection [1]
Cell Types: HT1376 cells have p53 mutations; MCR cells have two p53 mutations: one located in exon 4 (CGC→CCC) and one located in exon 9 (CAG→TAG) Tested Concentrations: 3 to 300 ng/mL Incubation Duration: 1, 6 and 24 hrs (hours) Experimental Results: IC50 was 90 ± 3 and 9.0 ± 0.4 ng/mL for MCR and HT1376 cells after 1 hour of treatment. After 24 hrs (hours) of treatment, the IC50 of MCR and HT1376 cells were 5.0±0.2 and 2.8±0.1 ng/mL, respectively. The growth inhibitory effect is dose-dependent and time-dependent. HT1376 cells were more sensitive than MCR cells, at least after short-term exposure. |
| Animal Protocol |
Animal/Disease Models: HT1376 model athymic Swiss nude mice [1]
Doses: 2 mg/kg Route of Administration: Oral treatment, once every four days for a total of four times. Experimental Results: Significant tumor growth inhibition was caused during the treatment period. |
| References | |
| Additional Infomation |
Gimatecan is an orally available 7-t-butoxyiminomethyl-substituted lipophilic camptothecin derivative.
Gimatecan is an orally bioavailable, semi-synthetic lipophilic analogue of camptothecin, a quinoline alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic and antiangiogenic activities. Gimatecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Although the mechanism of its antiangiogenic activity has yet to be full elucidated, this agent may inhibit endothelial cell migration, tumor neovascularization, and the expression of proangiogenic basic fibroblast growth factor (bFGF). |
| Molecular Formula |
C25H25N3O5
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|---|---|
| Molecular Weight |
447.4831
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| Exact Mass |
447.179
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| CAS # |
292618-32-7
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| PubChem CID |
9577124
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
780.6±70.0 °C at 760 mmHg
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| Flash Point |
425.9±35.7 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.667
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| LogP |
3.42
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
948
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC=CC=C5N=C4C3=C2)/C=N/OC(C)(C)C)O
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| InChi Key |
UIVFUQKYVFCEKJ-OPTOVBNMSA-N
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| InChi Code |
InChI=1S/C25H25N3O5/c1-5-25(31)18-10-20-21-16(12-28(20)22(29)17(18)13-32-23(25)30)15(11-26-33-24(2,3)4)14-8-6-7-9-19(14)27-21/h6-11,31H,5,12-13H2,1-4H3/b26-11+/t25-/m0/s1
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| Chemical Name |
(19S)-19-ethyl-19-hydroxy-10-[(E)-(2-methylpropan-2-yl)oxyiminomethyl]-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
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| Synonyms |
STI481; LBQ707
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~74.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2347 mL | 11.1737 mL | 22.3474 mL | |
| 5 mM | 0.4469 mL | 2.2347 mL | 4.4695 mL | |
| 10 mM | 0.2235 mL | 1.1174 mL | 2.2347 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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