LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells. LB-100 increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. LB-100 increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.
In vivo, LB-100 (2 mg/kg, i.p.) decreases in a time-dependent manner the activity of PP2A in xenografts and livers in nude mice. The combination of doxorubicin (1.5 kg/mL, every other day) and LB-100 (2 mg/kg, every other day) significantly slows the growth of tumors with reduction of tumor volume in two animals with no effects on tumor growth in animals treated with single agents.
|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.
|CAS Number||1026680-07-8; 1632032-53-1|
|Solubility||Water ≥ 40 mg/mL|
Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas.
Bai XL, et al. Mol Cancer Ther. 2014 Aug;13(8):2062-72. PMID: 24867249.
Dithiothreitol (DTT) is the common name for a small-molecule redox reagent known as Cleland's reagent; as a reducing or "deprotecting" agent for thiolated DNA.
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