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Merck
CN

5.38099

GS-493

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C21H14N6O8S
Molecular Weight:
510.44
NACRES:
NA.77
UNSPSC Code:
12352200

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assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

orange

solubility

DMSO: 1 mg/mL

Quality Level

100

Related Categories

General description

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 Actions

Cell permeable: yes
Primary Target
SHP2
Reversible: yes
Target IC50: 0.071, 2.08 & 3.17 &micro

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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