Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewAMG 510
Description: Potent and selective KRASG12C 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)
Biological Activity for AMG 510
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.
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 Data for AMG 510
| 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 560.6. 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for AMG 510
References for AMG 510
References are publications that support the biological activity of the product.
Lanman et al (2020) Discovery of a covalent inhibitor of KRASG12C (AMG 510) for the treatment of solid tumors. J.Med.Chem. 63 52 PMID: 31820981
Canon et al (2019) The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature 575 217 PMID: 31666701
If you know of a relevant reference for AMG 510, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: AMG 510, AMG 510 supplier, AMG510, KRASG12C, potent, selective, inhibitors, ERK, pERK, NSCLC, non, small, cell, lung, cancer, MEK, KRAS, G12C, Sotorasib, Ras, GTPases, 7713, Tocris Bioscience
Citations for AMG 510
Citations are publications that use Tocris products.
Currently there are no citations for AMG 510. Do you know of a great paper that uses AMG 510 from Tocris? Please let us know.
Reviews for AMG 510
There are currently no reviews for this product. Be the first to review AMG 510 and earn rewards!
Have you used AMG 510?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
RAS Oncoproteins Scientific Review
Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Pathways for AMG 510
Akt Signaling Pathway
The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.