AMG 510

Name: AMG 510
Brand: Tocris Bioscience
SKU: 7713

Tocris Bioscience, part of Bio-Techne | Catalog # 7713

Citations (2)

COA / SDS

Potent and selective KRASG12C inhibitor

Key Product Details

Description:	Potent and selective KRAS^G12C inhibitor
Alternative Names:	Sotorasib
Chemical Name:	(1R)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-4-[(2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]pyrido[2,3-d]pyrimidin-2(1H)-one
Purity:	≥98% (HPLC)
Molecular Weight:	560.6

View Full Technical Details for AMG 510

Technical Data
Citations

Biological Activity for AMG 510

AMG 510 is a potent and selective covalent KRAS^G12C inhibitor (IC₅₀ = 90 nM). Also a potent inhibitor of phospho-ERK (IC₅₀ = 68 nM). In an in vivo model of non-small cell lung cancer, AMG 510 causes regression of tumors, an increase in T-cell recruitment and a pro-inflammatory tumor microenvironment. Synergises with MEK inhibitors and Carboplatin (Cat. No. 2626) and is orally bioavailable.

Technical Data for AMG 510

M. Wt	560.6
Formula	C₃₀H₃₀F₂N₆O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2252403-56-6
PubChem ID	137278711
InChi Key	NXQKSXLFSAEQCZ-SFHVURJKSA-N
Smiles	O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=NC(C5=C(O)C=CC=C5F)=C(F)C=C42)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for AMG 510

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	56.06	100

Preparing Stock Solutions for AMG 510

The following data is based on the product molecular weight 560.6.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.78 mL	8.92 mL	17.84 mL
5 mM	0.36 mL	1.78 mL	3.57 mL
10 mM	0.18 mL	0.89 mL	1.78 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

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References for AMG 510

References are publications that support the biological activity of the product.

Canon The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature 2019 PMID: 31666701
Lanman Discovery of a covalent inhibitor of KRAS^G12C (AMG 510) for the treatment of solid tumors. J.Med.Chem. 2020 PMID: 31820981