BI-8128
BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
The BI-8128 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- CAS 番号: 2769714-36-3
- 分子式: C32H38N10O3
- 分子量:610.71
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
EGFR アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
EGFR (WT) 12 nM (IC50) |
EGFRT790M 6.7 nM (IC50) |
EGFRC797S 22 nM (IC50) |
EGFRdel19 T790M C797S 10 nM (IC50) |
EGFRL858R/T790M/C797S 3 nM (IC50) |
体外実験
BI-8128 potently inhibits the proliferation of Ba/F3 del19 EGFR cells (IC50 = 1.7 nM), and exhibits significant antiproliferative activity against other cell lines expressing EGFR mutants and wild-type (WT) EGFR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 2769714-36-3
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分子量 610.71
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分子式 C32H38N10O3
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SMILES
[H][C@@]12CN([C@@](CO1)(C2)[H])C3=C4N=C(N5CCN(CC5)CCOC)N(C4=CC(N6N=CC7=C(N=C(C8=C(C=CN=C8)OC)C=C67)C)=N3)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)