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BI-2865

Name: BI-2865
Brand: TargetMol
SKU: T72062
Price: 222 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T72062Cas No. 2937327-93-8

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

BI-2865

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Purity: 99.39%

Catalog No. T72062Cas No. 2937327-93-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$222	In Stock	In Stock
5 mg	$479	In Stock	In Stock
10 mg	$679	In Stock	In Stock
25 mg	$987	In Stock	In Stock
50 mg	$1,360	-	In Stock
100 mg	$1,850	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$489	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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Batch Information

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Purity:99.39%

Appearance:Solid

Color:White to Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]
Targets&IC50	KRas (G12C):4.5 nM (Kd), KRas (G12V):26 nM (Kd), KRas (G12D):32 nM (Kd), BaF3 cells:140 nM, KRas (G13D):4.3 nM (Kd), KRAS (WT):6.9 nM (Kd)
In vitro	METHODS: BaF3 cells expressing isogenic KRAS mutants of the indicated KRAS or expressing G12C, G12D or G12V mutant KRAS were treated in the absence of IL3 for 5 days to determine the effect on proliferation. RESULTS BI-2865 inhibited the proliferation of isogenic G12C, G12D or G12V mutant KRAS expressing BaF3 with an IC50 value of 140 nM. [1]

Chemical Properties

Molecular Weight	465.57
Formula	C₂₃H₂₇N₇O₂S
Cas No.	2937327-93-8
Smiles	C[C@]1(C2=C(SC(N)=C2C#N)CCC1)C3=NC(=NO3)C=4N=C(O[C@@H](C)[C@@]5(CCCN5C)[H])C=CN4
Relative Density.	1.38 g/cm3 at 20℃ (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 240 mg/mL (515.5 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1479 mL	10.7395 mL	21.4790 mL	107.3952 mL
5 mM	0.4296 mL	2.1479 mL	4.2958 mL	21.4790 mL
10 mM	0.2148 mL	1.0740 mL	2.1479 mL	10.7395 mL
20 mM	0.1074 mL	0.5370 mL	1.0740 mL	5.3698 mL
50 mM	0.0430 mL	0.2148 mL	0.4296 mL	2.1479 mL
100 mM	0.0215 mL	0.1074 mL	0.2148 mL	1.0740 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