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CL-387785

Chemical Structure : CL-387785

CAS No.: 194423-06-8

CL-387785 (EKI-785;WAY-EKI 785;CL387785;CL 387785;EKI785;WAY-EKI785;EKI 785)

Catalog No.: PC-42524Not For Human Use, Lab Use Only.

CL-387785 (EKI785, WAY-EKI785) is a specific, irreversible, covalent EGFR inhibitor with IC50 of 0.37 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CL-387785 (EKI785, WAY-EKI785) is a specific, irreversible, covalent EGFR inhibitor with IC50 of 0.37 nM.
CL-387785 blocks EGF-stimulated autophosphorylation of EGFR in A431 cells (IC50=5 nM).
CL-387785 inhibits cell proliferation (IC50= 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-ErbB2, and profoundly blocks the growth of a tumor that overexpresses EGFR in nude mice; orally active.

Physicochemical Properties

M.Wt 381.226
Formula C18H13BrN4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 13.67 mg/mL

Chemical Name/SMILES

2-Butynamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-

References

1. Discafani CM, et al. Biochem Pharmacol. 1999 Apr 15;57(8):917-25.

2. Kobayashi S, et al. Cancer Res. 2005 Aug 15;65(16):7096-101.

3. Kobayashi S, et al. Cancer Res. 2006 Dec 1;66(23):11389-98.

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