TTI-237 inhibited the binding of [(3)H]vinblastine to tubulin, but it caused a marked increase in turbidity development that more closely resembled the effect observed with docetaxel than that observed with vincristine. TTI-237 was active in vivo in several nude mouse xenograft models of human cancer, including LoVo human colon carcinoma and U87-MG human glioblastoma, when dosed i.v. or p.o.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
TTI-237: a novel microtubule-active compound with in vivo antitumor activity.
Beyer CF,et.al. Cancer Res 2008 Apr 1;2292-300. PMID: 18381436.
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Epothilone D is a potent microtubule stabilizer.
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Docetaxel trihydrate(Taxotere trihydrate), an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
Albendazole is a tubulin polymerization or assembly inhibitor, used for the treatment of a variety of parasitic worm infestations.
INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
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