>>Signaling Pathways>> Tyrosine Kinase>> EGFR>>BI-4020

BI-4020

Catalog No.GC38402

BI-4020은 4세대 경구 활성 및 비공유 EGFR 티로신 키나제 억제제입니다. BI-4020은 삼중 돌연변이 EGFR del19 T790M C797S 변이체(BaF3 세포주에서 IC50=0.2 nM)뿐만 아니라 이중 돌연변이 EGFR del19 T790M 및 1차 돌연변이 EGFR del19(IC50=1 nM)도 억제한다. BI-4020은 또한 EGFR wt(IC50=190nM)에 대한 활성을 보여줍니다. BI-4020은 높은 키놈 선택성과 우수한 DMPK 특성을 나타냅니다.

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 가격 재고 수량
1mg
US$324.00
재고 있음
5mg
US$1,020.00
재고 있음

Tel:(909) 407-4943 Email: sales@glpbio.com

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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. )

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

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리뷰

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

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