MAP855 - ≥99% , CAS No.1660107-77-6

CAS: 1660107-77-6 Cat. No.: M649236 分子式: C₂₈H₂₃ClF₂N₆O₃ 分子量: 564.97

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

概要

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

仕様と純度

≥99%

生化学的・生理学的メカニズム

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.

保管条件

Store at -20°C

入荷

Ice chest + Ice pads

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

純度

≥99%

名前と識別子

• 分子量: 564.97

化学的性質と物理的性質

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

よくある質問

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.