AMG 510
Tocris Bioscience, part of Bio-Techne | Catalog # 7713
Potent and selective KRASG12C inhibitor
Key Product Details
Description
Potent and selective KRASG12C inhibitor
Alternative Names
Sotorasib
Product Description
AMG 510 is a potent and selective covalent KRASG12C 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.Product Specifications
Molecular Weight
560.60
Formula
C30H30F2N6O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.06 | 100 |
Preparing Stock Solutions
for AMG 510
The following data is based on the product molecular weight 560.60
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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 KRASG12C (AMG 510) for the treatment of solid tumors. J.Med.Chem. 2020 PMID: 31820981
Product Specific Notices for AMG 510
For research use only
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