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VX-11e

Cat. No. M6235
VX-11e Structure
Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 145  USD145 In stock
25mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
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
Concentrations ~10 μM
Incubation time 48 h
Animal Experiment
Animal models NSG mice bearing human melanoma RPDX tumors
Formulation 5% ethanol, 20% propylene glycol, 7.4% Tween80
Dosages 50 mg/kg BID
Administration p.o.
Chemical Information
Molecular Weight 500.35
Formula C24H20Cl2FN5O2
CAS Number 896720-20-0
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Guo QS, et al. Sci Rep. Involvement of FAK-ERK2 signaling pathway in CKAP2-induced proliferation and motility in cervical carcinoma cell lines.

[2] Krepler C, et al. Clin Cancer Res. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies.

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Keywords: VX-11e supplier, ERK, inhibitors, activators


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