CL-387785 (EKI-785)

Catalog No.S7557 Synonyms: WAY-EKI 785

For research use only.

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

CAS No. 194423-06-8

Selleck's CL-387785 (EKI-785) has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NIH3T3 NXjYSJZjTnWwY4Tpc44h[XO|YYm= MoDETY5pcWKrdHnvckBw\iCHR1[gd5RqdXWuYYTl[EBpfW2jbjDldoJDOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJG5KUDOWMzDj[YxteyxiSVO1NF0xNjByMkZOwG0> NUDPdWF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0PFAzQDRpPkG2OFgxOjh2PD;hQi=>
A431 M3fNWWZ2dmO2aX;uJIF{e2G7 M3HkbmlvcGmkaYTpc44hd2ZiRVfGMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckBw\iCHR1\SJIlvKGi3bXHuJGE1OzFiY3XscJMtKEmFNUC9NE4xODYQvF2= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ{MUO5O{c,OjJ4MkGzPVc9N2F-
Sf9 NHXs[ZBHfW6ldHnvckBie3OjeR?= NHzNWVNVWF:WUlHOV3BQWlSHUkqg[YZndHW6IH;mJGhw\WOqc4SzN|M1OiCrbjDCR3JRNWW6cILld5NqdmdiU3[5JINmdGy|LDDJR|UxRTBwMt88US=> NUjiOGtPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxOVU5PDFpPkG1NVU2QDRzPD;hQi=>
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]

Protocol (from reference)

Kinase Assay: [1]
  • 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:[3] [4]
  • 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.
Animal Research:[5]
  • Animal Models: Human CRC cell line xenografts (nude mice)
  • Dosages: 100 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 63 mg/mL warmed
(165.25 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 381.23
Formula

C18H13BrN4O

CAS No. 194423-06-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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