MAP855 - ≥99% , CAS No.1660107-77-6

CAS: 1660107-77-6 Cat. No.: M649236 Formula: C₂₈H₂₃ClF₂N₆O₃ Molecular Weight: 564.97

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC 50 =3 nM, pERK EC 50 =5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2

In Vitro

MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC 50 =5 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay Cell Line: A375 cellsConcentration: 0-10 nM Incubation Time: 72 hours Result: Showed single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC 50 =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 . 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 . Pharmacokinetic Parameters of MAP855 in mouse, rat and dog . mouse rat dog CL [mL/min*kg] 32 35 22 V ss [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 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 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.

Form:Solid

IC50& Target:ERK 5 nM (EC 50 ) MEK1 3 nM (IC 50 )

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC 50 =3 nM, pERK EC 50 =5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥99%

Names and Identifiers

• Molecular Weight: 564.97

Chemical and Physical Properties

• Solubility: DMSO : 100 mg/mL (177.00 mM; Need ultrasonic)

Frequently Asked Questions

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1660107-77-6, the molecular formula is C28H23ClF2N6O3, and the molecular weight is 564.97 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.