AMG 510 |Covalent KRASG12C Inhibitor
Available Options
| Size | Price | Quantity | |
|---|---|---|---|
| 5mg | $69.00 | ||
| 25mg | $250.00 |
AMG 510 (2296729-00-3; Sotorasib) is a potent (IC50’s = 6 nM NCI-H358; 9 nM MIA PaCa-2) covalent KRASG12C inhibitor.1,2 It significantly inhibited tumor growth in NCI-H358 and MIA PaCa-2 cell lines as well as CT-26 tumors (mouse syngeneic model) and caused tumor regression at higher doses.1 AMG 510 improved the efficacy of various other chemotherapeutic agents including inhibitors of HER kinases, EGFR, SHP2, PI3K, AKT, and MEK 1,3 and synergized with immune checkpoint reagents1. FDA approved for use in KRASG12C-positive non-small cell lung cancer. AMG 510 displayed efficacy alone4,5 and in combination5 with trametinib and/or buparlisib in pancreatic ductal adenocarcinoma cell lines.
References/Citations:
- Canon et al. (2019), The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumor immunity; Nature 575 217
- Lanman et al. (2020); Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors, J. Med. Chem., 63 52
- Barrios-Bernal et al. (2023); A Novel Combination of Sotorasib and Metformin Enhances Cytotoxicity and Apoptosis in KRAS-Mutated Non-Small Cell Lung Cancer Cell Lines through MAPK and P70S6K Inhibition, Int. J. Mol. Sci., 24 4331
- Strickler et al. (2023); Sotorasib in KRASp.G12C-Mutated Advanced Pancreatic Cancer, N. Engl. J. Med., 388 33
- Ma et al. (2022); Inhibition of KRAS, MEKI, and PI3K Demonstrate Synergistic Anti-Tumor Effects in Pancreatic Ductal Adenocarcinoma Cell Lines, Cancers (Basel), 14 4467
C30H30F2N6O3
>98% HPLC
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
AMG 510 (2296729-00-3; Sotorasib) is a potent (IC50’s = 6 nM NCI-H358; 9 nM MIA PaCa-2) covalent KRASG12C inhibitor.1,2 It significantly inhibited tumor growth in NCI-H358 and MIA PaCa-2 cell lines as well as CT-26 tumors (mouse syngeneic model) and caused tumor regression at higher doses.1 AMG 510 improved the efficacy of various other chemotherapeutic agents including inhibitors of HER kinases, EGFR, SHP2, PI3K, AKT, and MEK 1,3 and synergized with immune checkpoint reagents1. FDA approved for use in KRASG12C-positive non-small cell lung cancer. AMG 510 displayed efficacy alone4,5 and in combination5 with trametinib and/or buparlisib in pancreatic ductal adenocarcinoma cell lines.
References/Citations:
- Canon et al. (2019), The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumor immunity; Nature 575 217
- Lanman et al. (2020); Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors, J. Med. Chem., 63 52
- Barrios-Bernal et al. (2023); A Novel Combination of Sotorasib and Metformin Enhances Cytotoxicity and Apoptosis in KRAS-Mutated Non-Small Cell Lung Cancer Cell Lines through MAPK and P70S6K Inhibition, Int. J. Mol. Sci., 24 4331
- Strickler et al. (2023); Sotorasib in KRASp.G12C-Mutated Advanced Pancreatic Cancer, N. Engl. J. Med., 388 33
- Ma et al. (2022); Inhibition of KRAS, MEKI, and PI3K Demonstrate Synergistic Anti-Tumor Effects in Pancreatic Ductal Adenocarcinoma Cell Lines, Cancers (Basel), 14 4467
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