RO4987655 (Synonyms: CH4987655)

Name: RO4987655
Brand: MedChemExpress
SKU: HY-14719
Rating: 5.0 (5 reviews)

Cat. No.: HY-14719 Purity: 99.26%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 874101-00-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 292	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 292	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 235	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 375	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1300	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE RO4987655

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MEK1 MEK2 MEK5 MEK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

Cellular Effect

Cell Line	Type	Value	Description	References
C32	IC₅₀	8.4 nM Compound: 24, CH4987655	Cytotoxicity against human C32 cells expressing b-Raf V600E mutant after 4 days Cytotoxicity against human C32 cells expressing b-Raf V600E mutant after 4 days	[PMID: 21316218]
COLO 205	IC₅₀	0.86 nM Compound: 24, CH4987655	Cytotoxicity against human COLO205 cells expressing b-Raf V600E mutant after 4 days Cytotoxicity against human COLO205 cells expressing b-Raf V600E mutant after 4 days	[PMID: 21316218]
HT-29	IC₅₀	1.7 nM Compound: 24, CH4987655	Cytotoxicity against human HT-29 cells expressing b-Raf V600E mutant after 4 days Cytotoxicity against human HT-29 cells expressing b-Raf V600E mutant after 4 days	[PMID: 21316218]
MIA PaCa-2	IC₅₀	3.3 nM Compound: 24, CH4987655	Cytotoxicity against human MIAPaCa2 cells expressing Kras G12C mutant after 4 days Cytotoxicity against human MIAPaCa2 cells expressing Kras G12C mutant after 4 days	[PMID: 21316218]
QG-56	IC₅₀	9.5 nM Compound: 24, CH4987655	Cytotoxicity against human QG56 cells expressing Hras Q61L mutant after 4 days Cytotoxicity against human QG56 cells expressing Hras Q61L mutant after 4 days	[PMID: 21316218]

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].

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

In Vivo

Single-agent oral administration of RO4987655 (CH4987655) results in complete tumor regressions in xenograft models. RO4987655 is rapidly absorbed with a t_max of ~1 h. Exposures are dose proportional from 0.5 to 4 mg. The disposition is biphasic with a terminal t_1/2 of ~25 hr. Intersubject variability is low, 9% to 23% for C_max 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 E_max model (E_max ~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].

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

Clinical Trial

Molecular Weight

565.28

Formula

C₂₀H₁₉F₃IN₃O₅

CAS No.

874101-00-5

Appearance

Solid

Color

White to off-white

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.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (176.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.26%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (252 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

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	[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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7690 mL	8.8452 mL	17.6903 mL	44.2259 mL
	5 mM	0.3538 mL	1.7690 mL	3.5381 mL	8.8452 mL
	10 mM	0.1769 mL	0.8845 mL	1.7690 mL	4.4226 mL
	15 mM	0.1179 mL	0.5897 mL	1.1794 mL	2.9484 mL
	20 mM	0.0885 mL	0.4423 mL	0.8845 mL	2.2113 mL
	25 mM	0.0708 mL	0.3538 mL	0.7076 mL	1.7690 mL
	30 mM	0.0590 mL	0.2948 mL	0.5897 mL	1.4742 mL
	40 mM	0.0442 mL	0.2211 mL	0.4423 mL	1.1056 mL
	50 mM	0.0354 mL	0.1769 mL	0.3538 mL	0.8845 mL
	60 mM	0.0295 mL	0.1474 mL	0.2948 mL	0.7371 mL
	80 mM	0.0221 mL	0.1106 mL	0.2211 mL	0.5528 mL
	100 mM	0.0177 mL	0.0885 mL	0.1769 mL	0.4423 mL

RO4987655 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RO4987655874101-00-5CH4987655RO 4987655RO-4987655CH 4987655CH-4987655MEKMitogen-activated protein kinase kinaseMAPKKMAP2KInhibitorinhibitorinhibit

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RO4987655 (Synonyms: CH4987655)

Customer Review

RO4987655 Related Antibodies

5 Publications Citing Use of MCE RO4987655

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MEK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

RO4987655 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

RO4987655 Related Classifications

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