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Setidegrasib (Synonyms: KRAS G12D inhibitor 17, ASP-3082, ASP3082)

Name: Setidegrasib
Brand: TargetMol
SKU: T74663
Price: 271 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T74663 Copy Product Info

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Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the formation of a ternary complex between KRAS G12D and the VHL E3 ubiquitin ligase, thereby facilitating the ubiquitination and proteasomal degradation of the oncogenic protein. Setidegrasib inhibits the levels of p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates antitumor activity in various mouse xenograft models of cancer. Setidegrasib can be used to study solid tumors with KRAS(G12D) mutations.

Setidegrasib

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Catalog No. T74663

Synonyms KRAS G12D inhibitor 17, ASP-3082, ASP3082

Cas No. 2821793-99-9

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Pack Size	Price	USA Stock	Global Stock
1 mg	$271	-	In Stock
5 mg	$597	-	In Stock
10 mg	$896	-	In Stock
50 mg	$1,970	-	In Stock

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

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

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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the formation of a ternary complex between KRAS G12D and the VHL E3 ubiquitin ligase, thereby facilitating the ubiquitination and proteasomal degradation of the oncogenic protein. Setidegrasib inhibits the levels of p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates antitumor activity in various mouse xenograft models of cancer. Setidegrasib can be used to study solid tumors with KRAS(G12D) mutations.
In vitro	Methods: Various KRAS(G12D)-mutant cancer cell lines (AsPC-1, PK-59, HPAC, GP2d, GP5d, etc.) and KRAS wild-type (WT) cell lines (A375, HT-29, BxPC-3, COLO-320) were treated with Setidegrasib (0.1 nM – 10 μM) for 6 days, and ATP levels were measured using the CellTiter-Glo 2.0 assay. Results: Setidegrasib potently inhibited the proliferation of multiple KRAS(G12D)-mutant cancer cell lines, whereas its activity against KRAS(WT) cells (A375, HT-29) and other KRAS mutants (G12V, G12C, G13D) was weaker (IC50 > 10 μM). [1]
In vivo	Methods: To investigate the antitumor activity of setidegrasib, an LXFA 1125 lung cancer PDX model (nude mice) was established. Setidegrasib (10, 30 mg/kg) was administered intravenously twice weekly for 21 days. Results: Setidegrasib inhibited tumor growth in a dose-dependent manner; IHC analysis revealed reduced KRAS(G12D) expression. [1]
Synonyms	KRAS G12D inhibitor 17, ASP-3082, ASP3082

Chemical Properties

Molecular Weight	1117.30
Formula	C₆₀H₆₅FN₁₂O₇S
Cas No.	2821793-99-9
Smiles	O(CC1=CC=C(C=C1)C2=CN([C@H](C(=O)N3[C@H](C(N[C@@H](CO)C4=CC=C(C=C4)C5=C(C)N=CS5)=O)C[C@@H](O)C3)[C@H](C)C)N=N2)C6=C(C(=CC7=C6N=C(OC8CCOCC8)N=C7N9[C@]%10(C[C@@](C9)(NC%10)[H])[H])C%11CC%11)C%12=C%13C(=CC(F)=C%12C)NN=C%13

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: 80.00 mg/mL (71.60 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8950 mL	4.4751 mL	8.9501 mL	44.7507 mL
5 mM	0.1790 mL	0.8950 mL	1.7900 mL	8.9501 mL
10 mM	0.0895 mL	0.4475 mL	0.8950 mL	4.4751 mL
20 mM	0.0448 mL	0.2238 mL	0.4475 mL	2.2375 mL
50 mM	0.0179 mL	0.0895 mL	0.1790 mL	0.8950 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