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Sotorasib

Name: Sotorasib
Brand: TargetMol
SKU: T8684
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8684Cas No. 2296729-00-3

Alias AMG-510

Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.

Sotorasib

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Purity: 99.95%

Catalog No. T8684Alias AMG-510Cas No. 2296729-00-3

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$31	In Stock	In Stock
2 mg	$44	In Stock	In Stock
5 mg	$72	In Stock	In Stock
10 mg	$128	In Stock	In Stock
25 mg	$237	In Stock	In Stock
50 mg	$393	In Stock	In Stock
100 mg	$483	In Stock	In Stock
500 mg	$1,080	In Stock	In Stock
1 g	$1,430	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$89	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.95%

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.
Targets&IC50	KRas (G12C) (CWH22 organoids):12.07 μM, KRas (G12C) (CLM22 organoids):10.95 μM
In vitro	METHODS: Twenty-two tumor cells were treated with Sotorasib (0-10 μM) for 72 h. Cell viability was measured using the CellTiter-Glo Luminescent Cell Viability Assay kit. RESULTS: Sotorasib impaired the growth of all KRAS G12C cell lines except SW1573, with IC50 values ranging from 0.004-0.032 μM. non-KRAS G12C cell lines were sensitive to Sotorasib, with an IC50 >7.5 μM. [1] METHODS: KRAS G12C mutant tumor cells were treated with Sotorasib (100 nM) for 4-72 h, and the expression levels of target proteins were detected using Western Blot method. RESULTS: Sotorasib rapidly inhibited KRAS downstream signaling, but p-ERK levels returned to 75% of the baseline level at 72 h. Sotorasib was also shown to rapidly inhibit KRAS downstream signaling. [2]
In vivo	METHODS: To assay antitumor activity in vivo, Sotorasib (3-100 mg/kg) was orally administered once daily for four weeks to athymic nude mice bearing the human pancreatic cancer tumor MIA PaCa-2 T2 or the human lung cancer tumor NCI-H358. RESULTS: Sotorasib significantly inhibited the growth of MIA PaCa-2 T2 and NCI-H358 tumors at all doses, and tumor regression was observed at higher doses. [1] METHODS: To assay antitumor activity in vivo, Sotorasib (30 mg/kg in 0.5% sodium carboxymethylcellulose, administered by gavage once daily) and Cisplatin (4 mg/kg in 0.9% saline, intraperitoneally every two days) were administered to Balb/C nude mice harboring human lung cancer tumors. RESULTS: Tumor shrinkage in the combination group was more than twice that of the single-administration group. [3]
Synonyms	AMG-510

Chemical Properties

Molecular Weight	560.594
Formula	C₃₀H₃₀F₂N₆O₃
Cas No.	2296729-00-3
Smiles	O=C1N=C(C=2C=C(F)C(=NC2N1C=3C(=NC=CC3C)C(C)C)C=4C(F)=CC=CC4O)N5CCN(C(=O)C=C)CC5C
Relative Density.	1.36 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 33.33 mg/mL (59.45 mM), when pH is adjusted to 11 with NaOH. Sonication is recommended.

DMSO: 247.5 mg/mL (441.5 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (8.92 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7838 mL	8.9191 mL	17.8382 mL	89.1911 mL
5 mM	0.3568 mL	1.7838 mL	3.5676 mL	17.8382 mL
10 mM	0.1784 mL	0.8919 mL	1.7838 mL	8.9191 mL
20 mM	0.0892 mL	0.4460 mL	0.8919 mL	4.4596 mL
50 mM	0.0357 mL	0.1784 mL	0.3568 mL	1.7838 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0178 mL	0.0892 mL	0.1784 mL	0.8919 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc