Home Cell Cycle Ras inhibitor BI-2852 For research use only.

BI-2852

BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.

BI-2852 Chemical Structure

BI-2852 Chemical Structure

CAS No. 2375482-51-0

Purity & Quality Control

BI-2852 Related Products

Signaling Pathway

Ras Signaling Pathways

Ras Signaling Pathway

Biological Activity

Description BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
Targets
GTP-KRASG12D [1]
(Cell-free assay)		 GTP-KRASG12D [1]
(Cell-free assay)
450 nM 750 nM(Kd)
In vitro
In vitro

BI-2852 is a KRAS inhibitor that binds with nanomolar affinity to a pocket, thus far perceived to be “undruggable,” between switch I and II on RAS. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitors because it binds to a different pocket present in both the active and inactive forms of KRAS. In doing so, it blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.[1]
Cell Research Cell lines NCI-H358 cells
Concentrations 3 μM, 10 μM, 30 μM, 50 μM
Incubation Time 0-24 hrs
Method

Cells are plated in 96 well plates (1500 cells per well) in the corresponding medium containing 10% FCS. The next day, compounds (Stock: 10 mM in 100% DMSO, including BI-2852), serially diluted in medium are added starting at 50 μM with 1:5 dilutions. Cells are incubated at 37 ℃ and 5% CO2 in a humidified atmosphere for 3 days. Quantification of living cells is performed using the cell titer glow reagent according to the manufacturer's recommendation. Luminescence is read in a 2030 VICTOR X5. Data are fitted by iterative calculation using a sigmoidal curve analysis program based on GraphPAD Prism with variable hill slope.

Chemical Information & Solubility

Molecular Weight 516.59 Formula

C31H28N6O2
CAS No. 2375482-51-0 SDF --
Smiles CN1C=C(N=C1)CN2C=CC3=C2C=C(C=C3)CNCC4=C(C5=CC=CC=C5N4)C6C7=C(C=CC(=C7)O)C(=O)N6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (193.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy BI-2852 | BI-2852 supplier | purchase BI-2852 | BI-2852 cost | BI-2852 manufacturer | order BI-2852 | BI-2852 distributor