CL-387785 (EKI-785)

Catalog No.S7557 Batch:S755703

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Technical Data

Formula

C18H13BrN4O
Molecular Weight 381.23 CAS No. 194423-06-8
Solubility (25°C)* In vitro DMSO 76 mg/mL (199.35 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 Assay:[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 Study:[5]
  • Animal Models

    Human CRC cell line xenografts (nude mice)

  • Dosages

    100 mg/kg

  • Administration

    i.p.

Customer Product Validation

, , Clin Cancer Res, 2015, 21(17):3913-23.

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

Cancer drug addiction is relayed by an ERK2-dependent phenotype switch [Kong X, et al. Nature, 2017, 550(7675):270-274] PubMed: 28976960
The soluble protease ADAMDEC1 released from activated platelets hydrolyzes platelet membrane pro-epidermal growth factor (EGF) to active high-molecular-weight EGF. [ J Biol Chem, 2017, 292(24):10112-10122] PubMed: 28455445
EGFR mutations and resistance to Irreversible pyrimidine based EGFR inhibitors. [Ercan D, et al. Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789] PubMed: 25948633
The inhibitory effect of CL-387785 on the invasion and metastasis of T790M EGFR mutant H1975 cells and its sensitization of radiotherapy [ Chinese Clinical Oncology, 2015, 7(7): 577] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.