2. MAPK/ERK Pathway Stem Cell/Wnt
  3. MEK ERK
  4. MAP855

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.

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MAP855 Chemical Structure

MAP855 Chemical Structure

CAS No. : 1660107-77-6

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5 mg USD 860 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2[1].

IC50 & Target

ERK

5 nM (EC50)

MEK1

3 nM (IC50)

In Vitro

MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC50=5 nM)[1].

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

MAP855 Related Antibodies

Cell Proliferation Assay

Cell Line: A375 cells[1]
Concentration: 0-10 nM
Incubation Time: 72 hours
Result: Showed single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC50=5 nM).
In Vivo

MAP855 (3 mg/kg for i.v., 10 mg/kg for p.o.; single) has good oral bioavailability and medium clearance in rodents[1].
MAP855 (30 mg/kg; p.o., b.i.d, 14 days) achieves comparable efficacy to trametinib dosed at the mouse MTD without any body weight loss[1].
Pharmacokinetic Parameters of MAP855 in mouse, rat and dog[1].

mouse rat dog
CL [mL/min*kg] 32 35 22
Vss [l/kg] 2.6 2.0 1.8
AUC po d.n. [μM*h] 0.4 0.6 1.4
Oral BAV [% F] 44 65 100

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

Animal Model: Male Wistar Rats[1]
Dosage: 3 mg/kg for i.v., 10 mg/kg for p.o.
Administration: i.v. and p.o., single
Result: Showed good oral bioavailability and medium clearance.
Animal Model: A375 Tumor Bearing Mice[1]
Dosage: 30 mg/kg
Administration: p.o., b.i.d, 14 days
Result: Achieved comparable efficacy to trametinib dosed at the mouse MTD without any body weight loss.
Molecular Weight

564.97

Formula

C28H23ClF2N6O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=NC2=C(C3=CC(C4=C(C=C(C=C4)OC5=NC=CC=N5)Cl)=C(F)C=C3N=C2)N1[C@]6([H])[C@H](CN(CC6)C(CO)=O)F
Shipping

Room temperature in continental US; may vary elsewhere.
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 : 100 mg/mL (177.00 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 1.7700 mL 8.8500 mL 17.7001 mL
5 mM 0.3540 mL 1.7700 mL 3.5400 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (4.43 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 (4.43 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.38%

COA (257 KB) HNMR (292 KB) RP-HPLC (248 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7700 mL 8.8500 mL 17.7001 mL 44.2501 mL
5 mM 0.3540 mL 1.7700 mL 3.5400 mL 8.8500 mL
10 mM 0.1770 mL 0.8850 mL 1.7700 mL 4.4250 mL
15 mM 0.1180 mL 0.5900 mL 1.1800 mL 2.9500 mL
20 mM 0.0885 mL 0.4425 mL 0.8850 mL 2.2125 mL
25 mM 0.0708 mL 0.3540 mL 0.7080 mL 1.7700 mL
30 mM 0.0590 mL 0.2950 mL 0.5900 mL 1.4750 mL
40 mM 0.0443 mL 0.2213 mL 0.4425 mL 1.1063 mL
50 mM 0.0354 mL 0.1770 mL 0.3540 mL 0.8850 mL
60 mM 0.0295 mL 0.1475 mL 0.2950 mL 0.7375 mL
80 mM 0.0221 mL 0.1106 mL 0.2213 mL 0.5531 mL
100 mM 0.0177 mL 0.0885 mL 0.1770 mL 0.4425 mL
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MAP855 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:

MAP8551660107-77-6MAP 855MAP-855MEKERKMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesMEK1MEK2pERKA375 cellsTumorOralSelectiveATP-competitiveInhibitorinhibitorinhibit

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