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RO4987655

Cat. No. M9014
RO4987655 Structure
Synonym:

CH4987655

Size Price Availability Quantity
5mg USD 315  USD315 In stock
10mg USD 550  USD550 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM. RO4987655 inhibits proliferation of NCI-H2122 cells in a dose-dependent manner with an IC50 value of 0.0065 μM.

In vivo, RO4987655 is rapidly absorbed with a tmax of ~1 h. Female athymic nude mice are randomized into study groups. The tumors size is estimated with digital caliper and PET scans performed on days 0, 1, and 3 with 1.0, 2.5, and 5.0 mg/kg RO4987655. The vehicle treatment does not inhibit the NCI-H2122 tumor xenograft growth over this time frame. In contrast, RO4987655 treatment results in 119% tumor growth inhibition (TGI) at 1.0 mg/kg, 145% TGI at 2.5 mg/kg and 150% TGI at 5.0 mg/kg on day 3.

Protocol
Cell Experiment
Cell lines human lung adenocarcinoma cell line NCI-H2122
Preparation method The human lung adenocarcinoma cell line NCI-H2122 are maintained in the designated media and indicated concentrations of heat-inactivated fetal bovine serum and L-glutamine. Cells are grown at 37°C in an atmosphere of 5%CO2. Cells are treated with various concentrations of RO4987655 (0.00001, 0.001, 0.1, and 10 μM) for 72 h in 96-well plates and viable cells were quantified with Cell Counting Kit-8.
Concentrations 0.00001, 0.001, 0.1, and 10 μM
Incubation time 72 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
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 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.

Chemical Information
Molecular Weight 565.28
Formula C20H19F3IN3O5
CAS Number 874101-00-5
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

[1] Tegnebratt T, et al. EJNMMI Res. Evaluation of efficacy of a new MEK inhibitor, RO4987655, in human tumor xenografts by [(18)F] FDG-PET imaging combined with proteomic approaches.

[2] Leijen S, et al. Clin Cancer Res. Phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of the MEK inhibitor RO4987655 (CH4987655) in patients with advanced solid tumors.

[3] Lee L, et al. Clin Cancer Res. The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RO4987655, CH4987655 supplier, MEK, inhibitors

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