5.38099

GS-493

• 別名: GS-493, 4-((2 Z)-2-(1,3- bis(4-Nitrophenyl)-5-oxo-1,5-dihydro-4H-pyrazol-4-yliden)hydrazino)benzenesulfonic acid, ( Z)-4-(2-(1,3- bis(4-Nitrophenyl)-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)benzenesulfonic acid, SHP2 Inhibitor VII
• 実験式（ヒル表記法）: C₂₁H₁₄N₆O₈S
• 分子量: 510.44
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange
• 溶解性: DMSO: 1 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable, bioavailable, non-toxic p-nitro analog of PHPS1 (Cat. No. 540213) that exhibits enhanced potency and selectivity. Acts as a phosphotyrosine mimetic, substrate-competitive and reversible catalytic domain inhibitor of SHP2 (IC₅₀ = 0.071, 2.08 & 3.17 µM for SHP2, SHP1 & PTP1B, respectively). Dose-dependently reverts HGF-stimulatd epithelial-mesenchymal transition of HPAF II cells and blocks human lung adenocarcinoma LXFA 526L anchorage-independent growth. Shown to significantly retard LXFA 526L xenografted tumor growth in mice (46 mg/kg/day, i.p., q.d.).

A cell-permeable, bioavailable, non-toxic p-nitro analog of PHPS1 (Cat. No. 540213) that exhibits enhanced potency and selectivity. Acts as a phosphotyrosine mimetic, substrate-competitive and reversible catalytic domain inhibitor of SHP2 (IC₅₀ = 0.071, 2.08 & 3.17 µM for SHP2, SHP1 & PTP1B, respectively). Dose-dependently reverts HGF-stimulatd epithelial-mesenchymal transition of HPAF II cells and blocks human lung adenocarcinoma LXFA 526L anchorage-independent growth. Shown to significantly retard LXFA 526L xenografted tumor growth in mice (46 mg/kg/day, i.p., q.d.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
SHP2

Reversible: yes

Target IC₅₀: 0.071, 2.08 & 3.17 &micro

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Grosskopf, S., et al. 2015. ChemMedChem.10, 815.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable