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pan-KRAS degrader 1

Name: pan-KRAS degrader 1
Brand: TargetMol
SKU: T200566
Price: 189 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T200566 Copy Product Info

Purity: 99.67%

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pan-KRAS degrader 1 is a pan-KRAS inhibitor with IC50 values of 29 nM and 9 nM against wild-type KRAS and G12V mutant respectively. It exerts anti-proliferative effects in KRAS-mutant cell lines and is suitable for lung cancer research.

Cas No. 2937327-83-6

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Pack Size	Price	USA Stock	Global Stock
1 mg	$189	-	In Stock
5 mg	$475	-	In Stock
10 mg	$766	-	In Stock
25 mg	$1,230	-	In Stock
50 mg	$1,860	-	In Stock
100 mg	$2,770	-	In Stock
1 mL x 10 mM (in DMSO)	$523	-	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:99.67%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	pan-KRAS degrader 1 is a pan-KRAS inhibitor with IC50 values of 29 nM and 9 nM against wild-type KRAS and G12V mutant respectively. It exerts anti-proliferative effects in KRAS-mutant cell lines and is suitable for lung cancer research.
Targets & IC50	KRas (G12V):9 nM, KRas (WT):29 nM
In vitro	Methods: Cell proliferation assays were performed to detect the inhibitory activity of pan-KRAS degrader 1 against KRAS-mutant cells. Its binding affinity to KRASG12V was determined, and its metabolic clearance properties in mouse and human liver microsomes were evaluated. Results: : 1.After 72 hours of treatment, pan-KRAS degrader 1 exhibited anti-proliferative activity against Ba/F3 KRASG12V and NCI-H727 cells, with EC₅₀ values of 0.959 μM and >1 μM, respectively. 2.pan-KRAS degrader 1 showed a high metabolic clearance rate in both mouse and human liver microsomes [1]. 3.pan-KRAS degrader 1 possessed high affinity for KRASG12V with an inhibition constant Ki of 25 nM [2].

Chemical Properties

Molecular Weight	450.56
Formula	C₂₂H₂₆N₈OS
Cas No.	2937327-83-6
Smiles	C[C@]1(C2=C(SC(N)=C2C#N)CCC1)C3=NC(=NO3)C4=NC(=NC=C4)N5[C@@H](C)CNCCC5

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 mg/mL (177.56 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2195 mL	11.0973 mL	22.1946 mL	110.9730 mL
5 mM	0.4439 mL	2.2195 mL	4.4389 mL	22.1946 mL
10 mM	0.2219 mL	1.1097 mL	2.2195 mL	11.0973 mL
20 mM	0.1110 mL	0.5549 mL	1.1097 mL	5.5487 mL
50 mM	0.0444 mL	0.2219 mL	0.4439 mL	2.2195 mL
100 mM	0.0222 mL	0.1110 mL	0.2219 mL	1.1097 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

Related Tags: pan-KRAS degrader 1 chemical structure | pan-KRAS degrader 1 in vitro | pan-KRAS degrader 1 formula | pan-KRAS degrader 1 molecular weight