In mice bearing 4T1 tumors, PND-1186 (100 mg/kg s.c.) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL for p.o.) also causes ovarian carcinoma tumor growth inhibition.Addition of PND-1186 to the drinking water of mice was well tolerated and inhibited ascites- and peritoneal membrane-associated ovarian carcinoma tumor growth associated with the inhibition of FAK Tyr-397 phosphorylation.
|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 24 mg/mL;Water <1 mg/mL|
|Source||Cell Death Differ (2017). Figure 8. PND-1186|
|Method||cell proliferation assay|
|Cell Lines||HCC cells|
|Incubation Time||48 h|
|Results||As expected, 1 μM PND-1186 significantly downregulated EZH2 mRNA and upregulated NOTCH2 expression|
PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments.
Tanjoni I,et.al. Cancer Biol Ther 2010 May 15;764-77. PMID: 20234191.
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