NSC87877

製品コードS8182 バッチS818201

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

C₁₉H₁₃N₃O₇S₂.2Na

分子量

503.42

CAS No.

56932-43-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (198.64 mM)

Water

100 mg/mL (198.64 mM)

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	NSC-87877は、SHP-1とSHP-2の両方を阻害する細胞透過性阻害剤であり、IC50値はそれぞれ355 nMと318 nMです。また、HEK293細胞におけるEGF誘導性のErk1/2活性化を阻害し、MDA-MB-468細胞の生存率/増殖を有意に低下させます。
in vitro	NSC-87877 seems to have no selectivity between human Shp2 and Shp1 in vitro. NSC-87877 inhibits EGF-stimulated Shp2 activation and EGF-induced Erk1/2 activation. NSC-87877 suppresses Erk1/2 activation by a Gab1-Shp2 chimera but does not affect PMA(phorbol 12-myristate 13-acetate)-induced Erk1/2 Activation. NSC-87877 does not inhibit EGF-induced Gab1 tyrosine phosphorylation and Gab1-Shp2 association. NSC-87877 can significantly reduce MDA-MB-468 cell viability/proliferation, especially in combination with a phosphoinositide 3-kinase inhibitor.
in vivo	NSC-87877 almost completely prevented EAE(experimental autoimmune encephalomyelitis) development by blocking the accumulation of inflammatory cells in the CNS(central nervous system). In an intrarenal mouse model of neuroblastoma, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. Intrathecal administration of NSC-87877 (an SHP2 antagonist; 1, 10, or 100 μM/rat) into the allodynic rats suppresses spinal nerve ligation-induced allodynia, spinal SHP2 and NR2B phosphorylation, and SHP2/phosphorylated SHP2-PSD-95 and PSD-95-NR2B/phosphorylated NR2B coprecipitation.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK293 cells
	濃度	50 μM
	反応時間	3 h
	実験の流れ	Serum-starved cells are pretreated with NSC-87877 (50 μM,3 h) or dimethyl sulfoxide (solvent) and then stimulated with EGF (100 ng/ml, 5 min) or left untreated. Cells are lysed in ice-cold PTP(protein tyrosine phosphatase) lysis buffer. Shp2 or Shp1 in cell lysate supernatants (0.5 mg/each) is immunoprecipitated with an antibody to Shp2 or an antibody to Shp1 plus protein A-Sepharose for 2 h at 4°C.
動物実験	動物モデル	C57BL/6 mice
	投薬量	2.5 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/16717135/
https://pubmed.ncbi.nlm.nih.gov/24372081/
https://pubmed.ncbi.nlm.nih.gov/26247726/

https://pubmed.ncbi.nlm.nih.gov/22425446/

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カスタマーフィードバック

: Data from [Data independently produced by , , Front Immunol, 2018, 9:2643]

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：

LILRB1-HLA-G axis defines a checkpoint driving natural killer cell exhaustion in tuberculosis [ EMBO Mol Med, 2024, 10.1038/s44321-024-00106-1]	PubMed: 39030302
Guided monocyte fate to FRβ/CD163+ S1 macrophage antagonises atopic dermatitis via fibroblastic matrices in mouse hypodermis [ Cell Mol Life Sci, 2024, 82(1):14]	PubMed: 39720957
Inhibition of PD-1 Alters the SHP1/2-PI3K/Akt Axis to Decrease M1 Polarization of Alveolar Macrophages in Lung Ischemia-Reperfusion Injury [ Inflammation, 2022, 10.1007/s10753-022-01762-6]	PubMed: 36357527
Resistance to allosteric SHP2 inhibition in FGFR-driven cancers through rapid feedback activation of FGFR. [ Oncotarget, 2020, 21;11(3):265-281]	PubMed: 32076487
Regulation of Microtubule Nucleation in Mouse Bone Marrow-Derived Mast Cells by Protein Tyrosine Phosphatase SHP-1 [ Cells, 2019, 8(4)]	PubMed: 30979083
Nogo-A/Pir-B/TrkB Signaling Pathway Activation Inhibits Neuronal Survival and Axonal Regeneration After Experimental Intracerebral Hemorrhage in Rats. [ J Mol Neurosci, 2019, 69(3):360-370]	PubMed: 31286407
CD180 Ligation Inhibits TLR7- and TLR9-Mediated Activation of Macrophages and Dendritic Cells Through the Lyn-SHP-1/2 Axis in Murine Lupus [Yang Y, et al. Front Immunol, 2018, 9:2643]	PubMed: 30498494

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。