1. MAPK/ERK Pathway
  2. MEK
  3. RO4987655

RO4987655 (Synonyms: CH4987655)

Cat. No.: HY-14719 Purity: 98.22%
Handling Instructions

RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.

For research use only. We do not sell to patients.

RO4987655 Chemical Structure

RO4987655 Chemical Structure

CAS No. : 874101-00-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 403 In-stock
Estimated Time of Arrival: December 31
2 mg USD 204 In-stock
Estimated Time of Arrival: December 31
5 mg USD 324 In-stock
Estimated Time of Arrival: December 31
10 mg USD 560 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2232 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.

IC50 & Target[1]

MEK1

5.2 nM (IC50)

MEK2

5.2 nM (IC50)

In Vitro

RO4987655 potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC50 of 5.2 nM for inhibition of MEK1/2[1]. RO4987655 inhibits proliferation of NCI-H2122 cells in a dose-dependent manner with an IC50 value of 0.0065 μM. RO4987655 at doses ranging from 0.1 to 1.0 μM suppresses pERK1/2 already at 2 h after the start of treatment[2].

In Vivo

Single-agent oral administration of RO4987655 (CH4987655) results in complete tumor regressions in xenograft models. RO4987655 is rapidly absorbed with a tmax of ~1 h. Exposures are dose proportional from 0.5 to 4 mg. The disposition is biphasic with a terminal t1/2 of ~25 hr. Intersubject variability is low, 9% to 23% for Cmax and 14% to 25% for area-under-the-curve (AUC). pERK inhibition is exposure dependent and is greater than 80% inhibition at higher doses. The pharmacokinetic-pharmacodynamic relationship is characterized by an inhibitory Emax model (Emax ~100%; IC50 40.6 ng/mL) using nonlinear mixed-effect modeling[1]. 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. PET imaging shows that [18F] FDG uptake in the xenografts decreases within 24 h (day 1) from the administration of RO4987655[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (70.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7690 mL 8.8452 mL 17.6903 mL
5 mM 0.3538 mL 1.7690 mL 3.5381 mL
10 mM 0.1769 mL 0.8845 mL 1.7690 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
Female athymic nude mice Balb nu/nu, age 5 to 6 weeks (18 to 22 g) are used. NCI-H2122 cells (4×106/mouse) are inoculated subcutaneously in the right flank of Balb-nu/nu mice. Once tumors are established (100 to 200 mm3), mice are randomized into groups with similar mean tumor volumes at the start of the study. 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. Tumor volume and body weight are measured on days 0 (baseline), 1, 2, 3, and 9 of [18F] FDG-PET imaging. Tumor growth inhibition is calculated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

565.28

Formula

C₂₀H₁₉F₃IN₃O₅

CAS No.

874101-00-5

SMILES

FC(C(F)=C(NC1=CC=C(I)C=C1F)C(C(NOCCO)=O)=C2)=C2CN3C(CCCO3)=O

Shipping

Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-14719