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BI-4020 EGFR inhibitor

Name: BI-4020
Brand: Selleck Chemicals
SKU: S8921
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8921

BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFR^{del19 T790M C797S} as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.

Chemical Structure

Molecular Weight: 542.68

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S892101 Ethanol]30 mg/mL]false]Water]20 mg/mL]false]DMSO]15 mg/mL]false Purity: 99.31%

99.31

Related Targets	VEGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
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Chemical Information, Storage & Stability

Molecular Weight	542.68	Formula	C₃₀H₃₈N₈O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2664214-60-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1CCCOC2=C(C=N[N]2C)C3=NC(=CC(=C3)C(=O)N=C4NC5=C(C=C(CN6CCN(C)CC6)C=C5)N4C1)C

Solubility

In vitro
Batch:

Ethanol : 30 mg/mL

Water : 20 mg/mL

DMSO : 15 mg/mL ( (27.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.	0.750mg/ml (1.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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.	0.750mg/ml (1.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 15 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.

Mechanism of Action

Targets/IC₅₀/Ki	EGFR^{del19 T790M C797S} ^[1] (anti-proliferation potency) 0.2 nM EGFR^{del19 T790M C797S} ^[1] (biomarker potency) 0.6 nM
In vitro	BI-4020 is a noncovalent, macrocyclic TKI, which inhibits not only the triple mutant EGFR^{del19 T790M C797S} variant but also the double mutant EGFR^{del19 T790M} and primary mutant EGFR^del19 while sparing activity against EGFR^wt.^[1]
In vivo	BI-4020 shows high potency on EGFR mutant cells, high kinome selectivity, and good DMPK properties, which leads to tumor regressions in the human PC-9 (EGFR^{del19 T790M C797S}) triple mutant NSCLC xenograft model in mice.^[1]
References	https://pubmed.ncbi.nlm.nih.gov/31689114/

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