AXL1717 (picropodophyllin, Picropodophyllotoxin, PPP) is a non-competitive, potent, and specific inhibitor of IGF-1Rα/β with IC50 of 1 nM. It exhibits little effect towards IR, FGFR, PDGFR and EGFR, and exerts no effects on microtubules and DNA topoisomerase II. Picropodophyllotoxin inhibits IGF1R autophosphorylation (IC50 ~ 1 nM), increases the fraction of cells in the G2/M phase and upregulates apoptosis.It also exhibits antiproliferative effects in multiple cancer cell lines (IC50 = 0.05 - 15 μM). In vivo,it has anticancer and antineovascularization activity.
|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||477-47-4; 17434-18-3|
Potent inhibitory effect of the cyclolignan picropodophyllin (PPP) on human adrenocortical carcinoma cells proliferation.
Doghman M, et al. Am J Cancer Res. 2011;1(3):356-361. PMID: 21968616.
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BMS-754807 is an ATP-competitive dual-kinase inhibitor of IGF-1R and IR with IC50s of 1.8 nM and 1.7 nM, respectively.
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