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

MAP855 

Cat. No.: HY-145702
Handling Instructions

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.

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

MAP855 Chemical Structure

MAP855 Chemical Structure

CAS No. : 1660107-77-6

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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].

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

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

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.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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MAP855
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HY-145702
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