CL-387785

CL-387785, also known as EKI-785 , is a n irreversible inhibitor of EGF-receptor (EGFR) kinase activity in vivo (IC50 = 250-490 pM). CL-387785 covalently bound to EGF-R. It also specifically inhibited kinase activity of the protein (IC50 = 370+/-120 pM), blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2, and profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80 mg/kg/day for 10 days, daily). CL-387,785 is useful for studying the interaction of small molecules with EGF-R and may have clinical utility.

Product information

CAS Number: 194423-06-8

Molecular Weight: 381.23

Formula: C18H13BrN4O

Synonym:

CL387785

EK-I785

CL 387785

CL-387785

EKI785

EK I785

Chemical Name: N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide

Smiles: CC#CC(=O)NC1C=CC2N=CN=C(NC3=CC(Br)=CC=C3)C=2C=1

InChiKey: BTYYWOYVBXILOJ-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Chiu HC, Chang TY, Huang CT, Chao YS, Hsu JT. EGFR and myosin II inhibitors cooperate to suppress EGFR-T790M-mutant NSCLC cells. Mol Oncol. 2012 Jun;6(3):299-310. doi: 10.1016/j.molonc.2012.02.001. Epub 2012 Feb 10. PubMed PMID: 22366308.
2. Chung JH, Rho JK, Xu X, Lee JS, Yoon HI, Lee CT, Choi YJ, Kim HR, Kim CH, Lee JC. Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs. Lung Cancer. 2011 Aug;73(2):176-82. doi: 10.1016/j.lungcan.2010.11.011. Epub 2010 Dec 17. PubMed PMID: 21168239.

Products are for research use only. Not for human use.