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KRA-533

Name: KRA-533
Brand: TargetMol
SKU: T38411
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T38411Cas No. 10161-87-2

Alias KRA533

KRA-533 is an effective KRAS agonist that targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This leads to accumulation of the active GTP-KRAS form, promoting apoptosis and autophagic death in cancer cells.

KRA-533

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Purity: 98.11%

Catalog No. T38411Alias KRA533Cas No. 10161-87-2

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$33	-	In Stock
5 mg	$52	-	In Stock
10 mg	$89	-	In Stock
25 mg	$189	-	In Stock
50 mg	$325	-	In Stock
100 mg	$553	-	In Stock
200 mg	$788	-	In Stock
1 mL x 10 mM (in DMSO)	$58	-	In Stock

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

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Purity:98.11%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	KRA-533 is an effective KRAS agonist that targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This leads to accumulation of the active GTP-KRAS form, promoting apoptosis and autophagic death in cancer cells.
In vitro	In HCC827 cells, KRA-533 (10 μM, 48 hours) significantly enhanced KRAS activity [1]. In H157 cells, the enhancement of KRAS activity by KRA-533 (0-15 μM, 48 hours) exhibited a dose-dependent effect. This effect was associated with elevated pERK levels, an increased ratio of active caspase 3/pro-caspase 3, and PARP cleavage, ultimately inducing apoptosis [1]. In H292 cells, KRA-533 (10 μM, 10 days) exhibited stronger growth inhibitory effects on KRAS-mutant cells compared to cells without KRAS mutations [1]. KRA-533 (5-15 μM) directly bound to wild-type (WT) KRAS protein as well as G12C, G12D, and G13D mutant KRAS proteins [1]. KRA-533 enhanced WT KRAS activity in a dose-dependent manner and further increased the activity of constitutively active KRAS mutants [1].
In vivo	In the KRAS mutant lung cancer xenograft model of Parazacco spilurus subsp. spilurus, KRA-533 (0-30 mg/kg, 28 days) administered via intraperitoneal injection demonstrated dose-dependent inhibition of tumor growth and dose-related induction of apoptosis and autophagy processes in tumor tissues [1]. KRA-533 exhibited optimal therapeutic indices within the dose range of 7.5 mg/kg to 30 mg/kg [1].
Synonyms	KRA533

Chemical Properties

Molecular Weight	314.18
Formula	C₁₃H₁₆BrNO₃
Cas No.	10161-87-2
Smiles	OC(=O)c1ccc(CCCCNC(=O)CBr)cc1

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 200 mg/mL (636.58 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1829 mL	15.9144 mL	31.8289 mL	159.1444 mL
5 mM	0.6366 mL	3.1829 mL	6.3658 mL	31.8289 mL
10 mM	0.3183 mL	1.5914 mL	3.1829 mL	15.9144 mL
20 mM	0.1591 mL	0.7957 mL	1.5914 mL	7.9572 mL
50 mM	0.0637 mL	0.3183 mL	0.6366 mL	3.1829 mL
100 mM	0.0318 mL	0.1591 mL	0.3183 mL	1.5914 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