Bevacizumab is A humanized IgG1 monoclonal antibody that binds with high affinity and specificity to all VEGF-A.
|Cell lines||NSCLC cell lines|
|Preparation method||Six NSCLC cell lines were seeded (~2,000–5,000 cells per well, depending on cell type) onto 96-well plates. After 24 h of incubation, cells were treated with erlotinib (0–20 µmol/L), bevacizumab (0–20 ng/mL) or a combination of these agents (erlotinib 1 µmol/L; bevacizumab 10 ng/mL) for 72 h in serum-containing medium. The viability was determined by MTS assay (Promega, Madison, WI) according to the manufacturer’s instructions.|
|Incubation time||72 h|
|Animal models||Female Wistar rats|
|Formulation||0.9%sodium chloride solution|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
 Lee AL, et al. Biomacromolecules. Injectable biodegradable hydrogels from vitamin D-functionalized polycarbonates for the delivery of avastin with enhanced therapeutic efficiency against metastatic colorectal cancer.
|Related VEGFR/PDGFR Products|
Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.
Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively.
SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM，while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities.
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