For research use only.
Molecular Weight(MW): 381.23
CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.
1 Customer Review
C, EGFR L718Q and L844V Ba/F3 cells retain sensitivity to irreversible quinazoline EGFR inhibitors. Cells were treated with different drugs at the indicated concentrations, and viable cells were measured after 72 hours of treatment and plotted relative to untreated controls. For Western blot analysis, 3T3 cells expressing the respective constructs were treated with different drugs at indicated concentrations for 16 hours. Cell extracts were immunoblotted to detect the indicated proteins. D, EGFR Del 1/L718Q Ba/F3 cells have a growth disadvantage. Equal number of cells was seeded in the presence of or absence of EGF or IL3. Cell number was evaluated in triplicate at the indicated time points.
Clin Cancer Res, 2015, 21(17):3913-23. . CL-387785 (EKI-785) purchased from Selleck.
Purity & Quality Control
Choose Selective EGFR Inhibitors
|Description||CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.|
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. 
|In vivo||In nude mice overexpressed EGF-R, CL-387785 (80 mg/kg/day, p.o.) profoundly blocks the growth of tumor.  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.  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. |
|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: ||
-  Discafani CM, et al. Biochem Pharmacol. 1999, 57(8), 917-925.
-  William E, et al. Kidney International. 2000, 57(1), 33-40.
-  Hama T, et al. Clin Exp Metastasis. 2012, 29(1), 19-25.
|In vitro||DMSO||63 mg/mL warmed (165.25 mM)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.