Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
Para uso exclusivo en investigación. No vendemos a pacientes.
Sotorasib Estructura química
No. CAS : 2296729-00-3
This product is a controlled substance and not for sale in your territory.
Sotorasib (1 μM) strongly downregulates survival protein Survivin in MIA PaCa-2 cells.
Powered by Bioz
See more details on Bioz
Ver todos los productos específicos de isoformas Ras:
Ver todas las isoformas
Descripciòn
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors[1][2].
IC50 & Target[1]
KRAS(G12C)
In Vitro
In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines[2]. ?
Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC50≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sotorasib Related Antibodies
Cell Viability Assay [3]
Cell Line:
NCI-H358 and MIA PaCa-2 cells
Concentration:
1-10 μM
Incubation Time:
72 hours
Result:
Potently impaired cellular viability in both NCI-H358 and MIA PaCa-2 (IC50≈0.006 μM and 0.009 μM respectively).
In Vivo
In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DMSO : 50 mg/mL (89.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.7838 mL
8.9192 mL
17.8383 mL
5 mM
0.3568 mL
1.7838 mL
3.5677 mL
10 mM
0.1784 mL
0.8919 mL
1.7838 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 20% HP-β-CD in Saline
Solubility: 10 mg/mL (17.84 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
[1]. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.
[2]. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.
[3]. Canon J, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223.
[Content Brief]
[4]. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors. Cancer Chemistry.
[1]. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.
[2]. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.
[3]. Canon J, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223.
[4]. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors. Cancer Chemistry.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O / DMSO
1 mM
1.7838 mL
8.9192 mL
17.8383 mL
44.5959 mL
5 mM
0.3568 mL
1.7838 mL
3.5677 mL
8.9192 mL
10 mM
0.1784 mL
0.8919 mL
1.7838 mL
4.4596 mL
15 mM
0.1189 mL
0.5946 mL
1.1892 mL
2.9731 mL
20 mM
0.0892 mL
0.4460 mL
0.8919 mL
2.2298 mL
25 mM
0.0714 mL
0.3568 mL
0.7135 mL
1.7838 mL
30 mM
0.0595 mL
0.2973 mL
0.5946 mL
1.4865 mL
40 mM
0.0446 mL
0.2230 mL
0.4460 mL
1.1149 mL
50 mM
0.0357 mL
0.1784 mL
0.3568 mL
0.8919 mL
DMSO
60 mM
0.0297 mL
0.1487 mL
0.2973 mL
0.7433 mL
80 mM
0.0223 mL
0.1115 mL
0.2230 mL
0.5574 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Sotorasib Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Teléfono : +1 850 650 7790