2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. 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.

BI-8128

BI-8128 Chemical Structure

CAS No. : 2769714-36-3

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BI-8128 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Description

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[1].

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.

BI-8128 Related Antibodies
Molecular Weight

610.71

Formula

C32H38N10O3
CAS No.
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.
Purity & Documentation
References
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BI-8128 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BI-81282769714-36-3BI8128BI 8128EGFREpidermal growth factor receptorErbB-1HER1T790M/C797S double mutationC797S EGFRepidermal growth factor receptorL858R/T790M/C797S EGFR kinaseWT EGFR kinaseATP-binding siteBa/F3 del19 EGFR cellsWT EGFR-expressing A431 cellsnon-small cell lung cancerInhibitorinhibitorinhibit

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