SCH772984

製品コードS7101 バッチS710105

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₃H₃₃N₉O₂
	分子量	587.67	CAS No.	942183-80-4
Solubility (25°C)*	体外	DMSO	14 mg/mL warmed with 50ºC water bath (23.82 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.
in vitro	SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. SCH772984 inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. SCH772984 also inhibits phosphorylation of residues in the activation loop of ERK itself. SCH772984 demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, SCH772984 effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. ^[1]
in vivo	SCH772984 induces tumor regressions in xenograft models at tolerated doses. SCH772984 effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models. ^[1]
特徴	Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity.

プロトコル(参考用のみ)

キナーゼアッセイ	ERK2 IMAP enzymatic assay
キナーゼアッセイ	SCH772984 is tested in 8 point dilution curves in duplicate against purified ERK2 or ERK1. The enzyme is added to the reaction plate. and incubated with the compound before adding a solution of substrate peptide and ATP. 14μl of diluted enzyme (0.3ng active ERK2 per reaction) is added to each well of a 384-well plate. The plates are gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction is stopped with 60μl of IMAP Binding Solution (1:2200 dilutions of IMAP beads in 1X Binding Buffer). The plates are incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates are read on the LJL Analyst.
細胞アッセイ	細胞株	BRAF-mutant or RAS-mutant tumor lines
	濃度	~10 μM
	反応時間	5 days
	実験の流れ	Cell proliferation experiments are performed in a 96-well format (six replicates), and cells are plated at 4,000/well density. At 24 h after cell seeding, cells are treated with DMSO or 9 point IC50 dilution (0.001-10 μM) at 1% DMSO final for all concentrations. Viability is assayed on 5 days after dosing using ViaLight luminescence kit following the manufacturer’s recommendations. For cell line panel viability assay, cells are treated with SCH772984 for 4 days and assayed by CellTiterGlo luminescent cell viability assay.
動物実験	動物モデル	Nude mice
	投薬量	12.5 mg/kg, 25 mg/kg, 50 mg/kg
	投与方法	i.p.

参考

[1] Morris EJ, et al. Cancer Discov, 2013 Apr 29.

カスタマーフィードバック

: Data from [Data independently produced by Leuk Lymphoma, 2014, 1, 8]

: , , Biochem Biophys Res Commun, 2017, 485(4):775-781

: Data from [Data independently produced by , , Nature, 2016, 534(7609):647-51]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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