CL-387785

CL-387785 (EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.

Product Specifications

CAS Number

[194423-06-8]

Product Name Alternative

EKI-785; WAY-EKI 785

UNSPSC

12352005

Hazard Statement

H315, H317, H318, H334, H335, H341, H361, H370, H413

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CL-387785.html

Purity

98.05

Solubility

DMSO : 13.67 mg/mL (ultrasonic; warming)

Smiles

O=C(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)C#CC

Molecular Formula

C18H13BrN4O

Molecular Weight

381.23

Precautions

H315, H317, H318, H334, H335, H341, H361, H370, H413

References & Citations

[1]Discafani CM, et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[ (3-bromophenyl) amino]-6-quinazolinyl]-2-butynamide (CL-387,785) . Biochem Pharmacol. 1999 Apr 15;57 (8) :917-25.|[2]Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57 (1) :33-40.|[3]Greulich H, et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2005 Nov;2 (11) :e313.|[4]Kobayashi S, et al. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res. 2005 Aug 15;65 (16) :7096-101.