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BI-4020

Catalog No.GC38402

A fourth-generation and non-covalent EGFR tyrosine kinase inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

BI-4020 Chemical Structure

Cas No.: 2664214-60-0

Size Price Stock Qty
1mg
$324.00
In stock
5mg
$1,020.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor, which inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM) whilst sparing activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].

BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM[1].

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].

[1]. Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.

Chemical Properties

Cas No. 2664214-60-0 SDF
Canonical SMILES O=C(C1=CC(C)=NC(C2=C(OCCC[C@@H](C)C3)N(C)N=C2)=C1)/N=C(N4)/N3C5=C4C=CC(CN6CCN(C)CC6)=C5
Formula C30H38N8O2 M.Wt 542.68
Solubility DMSO: 250 mg/mL (460.68 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8427 mL 9.2135 mL 18.4271 mL
5 mM 0.3685 mL 1.8427 mL 3.6854 mL
10 mM 0.1843 mL 0.9214 mL 1.8427 mL
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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.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 13 reference(s) in Google Scholar.)

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