5.38099

GS-493

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₁H₁₄N₆O₈S
• Molekulargewicht: 510.44
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: orange
• Löslichkeit: DMSO: 1 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
SHP2

Reversible: yes

Target IC₅₀: 0.071, 2.08 & 3.17 &micro

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable