Home Protein Tyrosine Kinase EGFR inhibitor CL-387785 (EKI-785) For research use only.

CL-387785 (EKI-785)

Synonyms: WAY-EKI 785

CL-387785 (EKI-785, WAY-EKI 785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.

CL-387785 (EKI-785) Chemical Structure

CL-387785 (EKI-785) Chemical Structure

CAS No. 194423-06-8

Purity & Quality Control

CL-387785 (EKI-785) Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NIH3T3 Function assay Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells, IC50=0.0025μM 16480284
A431 Function assay Inhibition of EGF-induced autophosphorylation of EGFR in human A431 cells, IC50=0.005μM 22621397
Sf9 Function assay TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells, IC50=0.2μM 15155841
Click to View More Cell Line Experimental Data

Biological Activity

Description CL-387785 (EKI-785, WAY-EKI 785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.
Targets
EGFR [1]
370 pM
In vitro
In vitro CL-387785 blocks EGF-stimulated autoposphorylation of the receptor in cells (IC50, 5 nM), In cell lines that overexpress EGF-R or c-erbB-2, CL-387785 inhibits cell proliferation (IC50, 31 nM) primarily in a cytostatic manner. [1]
Kinase Assay Liquid scintillation
Stock solutions of 500 μM CL-387785 (prepared in 100% DMSO) are diluted to the desired concentration with 30 mM HEPES, pH 7.4. Ten microliters of CL-387785 at various concentrations are incubated with 3 μL of recombinant enzyme (1:120 dilution in 100 mM HEPES, pH 7.4) on ice for 10 min. Then, 5 μL peptide (400 μM final concentration of RR-SRC composed of Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Ala-Ala-Arg-Gly), 10 μL of 4× reaction buffer containing 50 mM HEPES, pH 7.4, 80 μM ATP, 40 mM MnCl2, and 200 μM sodium orthovanadate. 0.30 μL [33P]ATP ( >2500 Ci/mmol), and 12 μL H2O are added. After incubation for 90 min at room temperature, the entire volume is spotted onto precut P81 filter papers. The filter discs are washed two times with 0.5% phosphoric acid, and radioactivity is measured using a liquid scintillation counter. Under these conditions, the specific activity of EGF-R kinase is approximately 0.50 pmol/mg/min.
Cell Research Cell lines Ba/F3-E709K, Ba/F3-l858r or Ba/F3-ERBB2 cells
Concentrations ~2000 nM
Incubation Time 2 days
Method MTS assays are performed with the CellTiter 96@ AQueous One solution proliferation kit. A total of 10,000 cells per well in 96-well flat-bottomed plates are incubated with various concentrations of inhibitors for 48 h. The IC50 is determined from dose–response curves using XLfit4.
In Vivo
In vivo In nude mice overexpressed EGF-R, CL-387785 (80 mg/kg/day, p.o.) profoundly blocks the growth of tumor. [1] In murine models of autosomal recessive polycystic kidney disease (ARPKD), treatment of Balb/c-bpk/bpk (BPK) mice with CL-387785 (90 mg/kg, i.p.) results in a marked reduction of collecting tubule cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and prolonged life span. [2] Doses of CL-387785 as low as 25 mg/kg reduces the growth of HCA-7-induced xenograft tumor, and a dose of 100 mg/kg prevents tumor growth entirely. Dose of 50 mg/kg CL-387785 is effective at reducing the growth of HCT-116-induced xenograft tumor. [5]
Animal Research Animal Models Human CRC cell line xenografts (nude mice)
Dosages 100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 381.23 Formula

C18H13BrN4O
CAS No. 194423-06-8 SDF Download CL-387785 (EKI-785) SDF
Smiles CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (199.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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