XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases. IGF1R is commonly activated in neoplastic growth and contributes to cell proliferation, cell survival, and resistance to genotoxic agents. SRC is a mediator of cell migration and invasion, key aspects of the metastatic phenotype. FGFR1-3 play important roles in tumor growth and angiogenesis. Aurora kinases control crucial steps in mitotic progression and cytokinesis.
|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.
The role of the insulin-like growth factor signaling pathway in non-small cell lung cancer and other solid tumors.
Scagliotti GV, et al. Cancer Treat Rev. 2012 Jun;38(4):292-302. PMID: 21907495.
|Related IGF-1R Products|
Picropodophyllotoxin is an insulin-like growth factor-I (IGF-I) receptor kinase inhibitor.
NVP-AEW541 is a novel, potent and selective inhibitor of IGF-IR kinase with IC50 value of 0.086.
AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).
AXL1717 (picropodophyllin, Picropodophyllotoxin, PPP) is a non-competitive, potent, and specific inhibitor of IGF-1Rα/β with IC50 of 1 nM.
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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