SCH772984

製品コードS7101 バッチS710106

印刷

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 (warmed with 50ºC water bath)

6 mg/mL (10.2 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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は、細胞フリーアッセイにおいてそれぞれ4 nMおよび1 nMのIC50値を持つ、ERK1/2の新規特異的阻害剤であり、RASまたはBRAF変異がん細胞において強力な有効性を示します。
in vitro	SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. This compound inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. It also inhibits phosphorylation of residues in the activation loop of ERK itself. This inhibitor demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, it effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors.
in vivo	SCH772984 induces tumor regressions in xenograft models at tolerated doses. This compound effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models.
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 this 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 this compound 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

https://pubmed.ncbi.nlm.nih.gov/23614898/

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Macropinocytosis maintains CAF subtype identity under metabolic stress in pancreatic cancer [ Cancer Cell, 2025, S1535-6108(25)00271-5]	PubMed: 40712568
Macrophage-derived amphiregulin induces myofibroblast transition in adipogenic lineage precursors near Staphylococcus aureus abscess in bone marrow [ Nat Commun, 2025, 16(1):8409]	PubMed: 40998791
mTORC1 cooperates with tRNA wobble modification to sustain the protein synthesis machinery [ Nat Commun, 2025, 16(1):4201]	PubMed: 40328729
Orosomucoid 1 Ameliorates Temporomandibular Joint Osteoarthritis by Maintaining Cartilage Homeostasis [ Adv Sci (Weinh), 2025, 12(36):e00028]	PubMed: 40583170
EGFR TKIs suppress MUC1 glycosylation through the PI3K/AKT/SP1/C1GALT1 pathway to enhance TnMUC1 CAR-T efficacy in EGFR-mutant NSCLC [ Cell Rep Med, 2025, S2666-3791(25)00272-1]	PubMed: 40562040
Tumorigenesis Driven by BRAFV600E Requires Secondary Mutations that Overcome it's Feedback Inhibition of RAC1 and Migration [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220]	PubMed: 39992718
Targeting CLEC4E in immunosuppressive tumour-associated macrophages via BET inhibition [ Clin Transl Med, 2025, 15(10):e70505]	PubMed: 41088887
Enhancing CAR-T Cell Metabolic Fitness and Memory Phenotype for Improved Efficacy against Hepatocellular Carcinoma [ Int J Biol Sci, 2025, 21(9):4231-4251]	PubMed: 40612678
Opposing roles for GSK3β and ERK1-dependent phosphorylation of huntingtin during neuronal dysfunction and cell death in Huntington's disease [ Cell Death Dis, 2025, 16(1):328]	PubMed: 40263294
ERK activation waves coordinate mechanical cell competition leading to collective elimination via extrusion of bacterially infected cells [ Cell Rep, 2025, 44(1):115193]	PubMed: 39817903

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。