XL647 is an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression. Check for active clinical trials or closed clinical trials using this agent.Inhibition of EGFR blocks signal transduction and thus impedes vascularization. XL647 inhibits other receptor tyrosine kinases such as Neu (ErbB2), Flk-1 (KDR), EphB4, and Flt-4. XL647 administered on an intermittent or daily-dosing schedule demonstrated antitumor activity in patients with EGFR-activating mutations. The adverse-event profile was similar for the two dosing schedules.
|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||781613-23-8 (874286-84-7)|
|Solubility||DMSO 3 mg/mL|
Phase II study of the multitargeted tyrosine kinase inhibitor XL647 in patients with non-small-cell lung cancer.
Pietanza MC, et al. J Thorac Oncol. 2012 May;7(5):856-65. PMID: 22722787.
EGFR-mutant lung adenocarcinomas treated first-line with the novel EGFR inhibitor, XL647, can subsequently retain moderate sensitivity to erlotinib.
Chmielecki J, et al. J Thorac Oncol. 2012 Feb;7(2):434-42. PMID: 22173702.
XL647--a multitargeted tyrosine kinase inhibitor: results of a phase II study in subjects with non-small cell lung cancer who have progressed after responding to treatment with either gefitinib or erlotinib.
Pietanza MC, et al. J Thorac Oncol. 2012 Jan;7(1):219-26. PMID: 22011666.
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