In vitro: In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM.
In vivo: In both rats and mice, VX-11e shows good oral bioavailability. In NSG mice bearing human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth. When used in combination with BKM120, VX-11e results in significantly improved tumor growth inhibition.
|Cell lines||HT29 cells|
|Preparation method||Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter. The IC50 is the 50% inhibition of contr|
|Incubation time||48 h|
|Animal models||NSG mice bearing human melanoma RPDX tumors|
|Formulation||5% ethanol, 20% propylene glycol, 7.4% Tween80|
|Dosages||50 mg/kg BID|
|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||100 mg/mL in DMSO|
Involvement of FAK-ERK2 signaling pathway in CKAP2-induced proliferation and motility in cervical carcinoma cell lines.
Guo QS, et al. Sci Rep. 2017 May 18;7(1):2117. PMID: 28522860.
Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies.
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