Home Tools

Cart

RO4987655

Catalog No. T5412 CAS 874101-00-5

Synonyms: CH4987655, RG7167

RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

RO4987655, CAS 874101-00-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 113.00
2 mg	In stock	$ 167.00
5 mg	In stock	$ 267.00
10 mg	In stock	$ 463.00
25 mg	In stock	$ 748.00
50 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 333.00

Bulk Inquiry

Select Batch

Purity: 98.21%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).
Targets&IC50	MEK2:5.2 nM (cell free), MEK1:5.2 nM (cell free)
In vitro	CH4987655 (RO4987655) potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC50 of 5.2 nmol/L for inhibition of MEK1/2 [1]. In NCI-H2122 cells, RO4987655 at doses ranging from 0.1 to 1.0 μM suppressed pERK1/2 already at 2 h after the start of treatment. RO4987655 inhibited proliferation of NCI-H2122 cells in a dose-dependent manner with an IC50 value of 0.0065 μM [2].
In vivo	In the dose-ranging study, treatment with RO4987655 5.0 mg/kg led to dramatic decrease in FDG uptake on day 1. The daily RO4987655, 2.5 mg/kg treatment were followed by PET examinations on days 1, 3, and 9 of the drug administration. The maximum decrease was observed on day 1, followed by a slight rebound on day 3. The effect plateaued thereafter to day 9 of treatment [2]. Doses of 0.5, 1, 2, 3, and 4 mg were safe and well-tolerated. A total of 26 adverse events (n = 15) were reported: 21 mild, 5 moderate, and none severe. Moderate adverse events were experienced by one subject at 1 mg (autonomic nervous system imbalance) and three subjects at 4 mg (diarrhea, abdominal pain, autonomic nervous system, and acne) [3].
Cell Research	Cells were treated with various concentrations of RO4987655 for 72 h in 96-well plates and viable cells were quantified with Cell Counting Kit-8. For Western blotting, cells were treated with RO4987655 for indicated periods and lysed with cell lysis buffer containing a protease inhibitor cocktail, phosphatase inhibitor cocktails 2 and 3, and 1 mM PMSF. For detection of protein bands, the following were used as primary antibodies: pEGFR, EGFR, pMKK4, MKK4, pAKT, AKT, pERK, ERK, pMEK1/2, MEK, Cyclin D1, and actin. All protein bands were visualized with secondary antibodies labeled with HRP and ECL system by using ImageQuant LAS 4000 [2].
Animal Research	A time interval of 20 to 24 h was used between daily RO4987655 administration and completion of PET imaging for each tumor-bearing mouse and for each PET imaging time point (day 0, 1, 3 and 9). Mice were fasted for 6 to 8 h prior to start of the imaging session. [18F] FDG (7 to 8 MBq per mouse, maximum volume of 200 μL) was administered to awake, warmed (37°C) mice by a bolus injection via the tail vein. Forty to sixty minutes after the tracer injection, the mice were administered with isoflurane, controlled by an E-Z anesthesia vaporizer. The mice were placed on a heated pad (37°C) on the camera bed, with most of the body volume in the field of view (7.68 cm). Emission data were collected for 20 min in list mode with a microPET Focus 120 scanner. Maximum standardized uptake values (SUVmax) of [18F] FDG uptake in the tumor were calculated and normalized to the administered activity (MBq/body weight, g). The drug effect on tumor metabolism was estimated as%SUVmax change to day 0 (baseline) [2].

Synonyms	CH4987655, RG7167
Molecular Weight	565.28
Formula	C20H19F3IN3O5
CAS No.	874101-00-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 35 mg/mL (61.92 mM)

References and Literature

1. Lee L, et al. The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of CH4987655 in healthy volunteers: target suppression using a biomarker. Clin Cancer Res. 2009 Dec 1;15(23):7368-74. 2. Tegnebratt T, et al. Evaluation of efficacy of a new MEK inhibitor, RO4987655, in human tumor xenografts by [(18)F] FDG-PET imaging combined with proteomic approaches. EJNMMI Res. 2014 Dec;4(1):34.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Clinical Compound Library NO PAINS Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets

SCH772984 Trametinib (DMSO solvate) Lidocaine hydrochloride Binimetinib CI-1040 Boehmenan Honokiol URMC-099

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RO4987655 874101-00-5 MAPK MEK RG 7167 CH 4987655 RO 4987655 MAPKK Mitogen-activated protein kinase kinase MAP2K RO-4987655 Inhibitor CH4987655 inhibit RG-7167 RG7167 CH-4987655 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.