CL-387785

• CAT Number: I002482
• CAS Number: 194423-06-8
• Molecular Formula: C₁₈H₁₃BrN₄O
• Molecular Weight: 381.23
• Purity: ≥95%
• Synonyms: N-(4-((3-bromophenyl)amino)quinazolin-6-yl)but-2-ynamide
• Target: Protein Tyrosine Kinase/RTK
• Solubility: DMSO: ≤ 13.67 mg/mL
• Storage: Store at -20°C
• IC50: 370+/-120 pM
• InChI: InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
• InChIKey: BTYYWOYVBXILOJ-UHFFFAOYSA-N
• SMILES: CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br

CL-387785 (CAT: I002482), also known as EKI785 or WAY-EKI 785, is an irreversible inhibitor of the epidermal growth factor receptor (EGFR). It selectively targets EGFR and forms a covalent bond with the receptor, leading to the inhibition of EGFR signaling. By blocking EGFR, CL-387785 can impede cellular processes involved in cell growth, proliferation, and survival. This compound has been investigated for its potential therapeutic applications in cancer treatment, particularly in tumors driven by aberrant EGFR signaling.

Reference

[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.