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VX-11e

Cat. No. M6235
VX-11e Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 175 In stock
50mg USD 465 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 500.35
Formula C24H20Cl2FN5O2
CAS Number 896720-20-0
Purity >98%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

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.
Krepler C, et al. Clin Cancer Res. 2016 Apr 1;22(7):1592-602. PMID: 26673799.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: VX-11e supplier, ERK, inhibitors

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