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.
For research use only. We do not sell to patients.
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 No.: 2769714-36-3
- Formula: C32H38N10O3
- Molecular Weight:610.71
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All EGFR Isoforms
More
Biological Activity
Description
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) |
In Vitro
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.
Chemical Information
-
CAS No. 2769714-36-3
-
Molecular Weight 610.71
-
Formula C32H38N10O3
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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.
-
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BI-8128 Related Classifications
HY-171884 Related Classifications
Powered by Bioz