SCH772984

製品コードS7101 バッチS710108

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)

25 mg/mL (42.54 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.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.600mg/ml (1.02mM)	Taking the 1 mL working solution as an example, add 100 μL of 6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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：

Antileukemic activity and mechanism of action of the novel PI3K and histone deacetylase dual inhibitor CUDC-907 in acute myeloid leukemia [ Haematologica, November 2019, 2225-2240]	PubMed: 30819918
Inhibition of ERK1/2 in cancer-associated pancreatic stellate cells suppresses cancer–stromal interaction and metastasis [ Journal of Experimental & Clinical Cancer Research, May 27, 2019, 221]	PubMed: 31133044
In Vivo E2F Reporting Reveals Efficacious Schedules of MEK1/2–CDK4/6 Targeting and mTOR–S6 Resistance Mechanisms [ Cancer Discovery, May 2018, 568-581]	PubMed: 29496664
Small-molecule inhibition of MAP2K4 is synergistic with RAS inhibitors in KRAS-mutant cancers [ PNAS, February 20, 2024, e2319492121]	PubMed: 38377196
Proteomic and Transcriptomic Profiling Identifies Mediators of Anchorage-Independent Growth and Roles of Inhibitor of Differentiation Proteins in Invasive Lobular Breast Cancer [ bioRxiv, February 07, 2019, 543132]
Loss of EGFR confers acquired resistance to AZD9291 in an EGFR-mutant non-small cell lung cancer cell line with an epithelial–mesenchymal transition phenotype [ Journal of Cancer Research and Clinical Oncology, August 2018, 1413-1422]
The phosphoinositide-3 kinase (PI3K)-δ,γ inhibitor, duvelisib shows preclinical synergy with multiple targeted therapies in hematologic malignancies [ PLOS One, August 01, 2018, e0200725]
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

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。