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(S)-AMG-510

Name: (S)-AMG-510
Brand: TargetMol
SKU: T22258
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Synonyms:

Catalog No. T22258 Copy Product Info

Purity: 99.76%

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(S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C through covalent interaction with mutant cysteine, thereby promoting clinical efficacy in KRASG12C tumors.

Cas No. 2252403-56-6

Pack Size	Price	USA Stock	Global Stock
2 mg	$31	In Stock	In Stock
5 mg	$48	In Stock	In Stock
10 mg	$77	In Stock	In Stock
25 mg	$158	In Stock	In Stock
50 mg	$288	In Stock	In Stock
100 mg	$449	In Stock	In Stock
500 mg	$987	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$70	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.76%

Appearance:Solid

Color:White to Yellow

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COA LCMS HNMR HPLC

Product Introduction

(S)-AMG-510 AI Summary

(S)-AMG-510 exhibits potent bioactivity related to the inhibition of KRAS G12C mutants in various human cancer cell lines. It demonstrates strong antiproliferative activity, particularly against NCI-H358 and MIA PaCa-2 cells, with IC50 values as low as 6.4 nM and 22.0 nM respectively. The compound effectively inhibits ERK phosphorylation, SOS1/KRAS protein-protein interactions, and displays a Kinact/Ki ratio of 9.9 /mM/s. In in vivo models, (S)-AMG-510 shows promising antitumor effects in xenografted mice and moderate oral bioavailability. It has good solubility across various buffers, exhibits protein binding in plasma, and is cleared in different animal models..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	(S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C through covalent interaction with mutant cysteine, thereby promoting clinical efficacy in KRASG12C tumors.
In vitro	METHODS: KRAS G12 mutant NSCLC cell lines (NCI-H358 [G12C], NCI-H23 [G12C], NCI-H2122 [G12C], A549 [G12S], NCI-H2009 [G12A], NCI-H441 [G12V], and SK-LU1 [G12D]) were treated with (S)-AMG-510 (0.001-100000nM, 72 hours), and cell viability was detected by CCk8. RESULTS All non-G12C cell lines were as expected. Among KRAS G12 C cells, H358 and H2122 were sensitive, but H23 cells were resistant to (S)-AMG-510. METHODS: Engineered Ba/F3 cells carrying KRAS G12C were treated with (S)-AMG-510 (0.001-100000nM, 72 hours), and cell viability was determined by CCK8. RESULTS Ba/F3 cells expressing KRAS G12C were sensitive to sotorasib with an IC50 value of 12.4nM. METHODS: Ba/F3 cells expressing KRAS G12C or G12D were treated with (S)-AMG-510 (10-100nM, 6 hours) or adagrasib and immunoblotted. RESULTS (S)-AMG-510 inhibited pERK and pS6 levels in Ba/F3 cells expressing KRAS G12C; it had no effect on KRAS G12D. [3]
In vivo	METHODS: (S)-AMG-510 (10 mg/kg, oral) or sotorasib (10 mg/kg) + encorafenib (20 mg/kg) were used to treat NOD/SCID mice bearing tumor xenografts. The body weight and tumor size of the mice were monitored every 2 days. RESULTS (S)-AMG-510 withdrawal and the combination of BRAF inhibitors induced tumor regression in vivo. [4]

Chemical Properties

Molecular Weight	560.594
Formula	C₃₀H₃₀F₂N₆O₃
Cas No.	2252403-56-6
Smiles	O=C1N(C=2C(C(=N1)N3[C@@H](C)CN(C(C=C)=O)CC3)=CC(F)=C(N2)C4=C(F)C=CC=C4O)C5=C(C(C)C)N=CC=C5C
Relative Density.	1.36 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 25 mg/mL (44.6 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: < 2.5 mg/mL (4.46 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (4.46 mM), Solution.

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

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

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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