LY573636 is a novel anticancer agent that induces apoptosis through the intrinsic pathway and has antiangiogenic activity in preclinical models. LY573636 demonstrated activity across a broad range of tumors, including melanoma. LY573636 causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY573636 administered at a targeted C(max) of 420 μg/mL on Day 1 of 21-day cycles demonstrated activity and tolerable toxicity as second-line treatment in malignant melanoma. LY573636 is selectively toxic towards tumor cells over their normal counterparts.
|Source||Mol Cancer Ther (2011). Figure 1. LY 573636|
|Cell Lines||Calu-6 and A-375 cell|
|Concentrations||from 200 mmol/L to approximately 200 nmol/L|
|Incubation Time||72 hours|
|Results||Fluorescence-activated cell sorting (FACS) analysis of Calu-6 and A-375 cell lines showed that tasisulam induced a concentration-dependent increase in 4N DNA|
|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.
|Solubility||DMSO 43 mg/mL|
A phase 2 study of tasisulam sodium (LY573636 sodium) as second-line treatment for patients with unresectable or metastatic melanoma.
Kirkwood JM, et al. Cancer. 2011 Oct 15;117(20):4732-9. PMID: 21456002.
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