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BI-2865 KRAS inhibitor

Name: BI-2865
Brand: Selleck Chemicals
SKU: E1474
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1474

BI-2865 is a none-covalent pan-KRAS Inhibitor. It binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively and inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 ce

Chemical Structure

Molecular Weight: 465.57

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Quality Control

Batch: E147401 DMSO]93 mg/mL]false]Ethanol]93 mg/mL]false]Water]Insoluble]false Purity: 99.01%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.01

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras Aurora Kinase Casein Kinase
Other KRas Inhibitors	RMC-7977 Daraxonrasib (RMC-6236) MRTX1133 Zoldonrasib (RMC-9805) BI-2852 Adagrasib (MRTX849) HRS-4642 ARS-1620 BI-3406 ARS-853

Q&A of BI-2865: Insights Rooted in Extensive Publications, Every Answer Cited

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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 93 mg/mL (199.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.650mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 93 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.150mg/ml (2.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Search directly for a cell line, or select a cell line to find matched working concentrations

BI-2865 is a potent inhibitor of P-gp (0.3 µM), KRAS (4.3 nM). BI-2865 exhibits the greatest inhibitory potency toward KRAS (IC50 = 4.3 nM).

Mechanism of Action

Information	BI-2865 is a potent KRAS/P-gp inhibitor. It affects ERK/AKT signaling pathways, by reducing KRAS-GTP, inhibiting MDR and growth.
Read more about BI-2865 IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	465.57	Formula	C₂₃H₂₇N₇O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2937327-93-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

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Handling Instructions

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