CL-387785 (EKI-785) EGFR inhibitor

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Quality Control

Batch: Purity: 99.79%

99.79

Related Targets	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other EGFR Inhibitors	Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) Genistein

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	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

Chemical Information, Storage & Stability

Molecular Weight	381.23	Formula	C₁₈H₁₃BrN₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	194423-06-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	WAY-EKI 785			Smiles	CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br

Solubility

In vitro
Batch:

DMSO : 76 mg/mL (199.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (7.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (7.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 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.

Mechanism of Action

Targets/IC₅₀/Ki	EGFR 370 pM
In vitro	CL-387785 (EKI-785) blocks EGF-stimulated autophosphorylation of the receptor in cells (IC50, 5 nM). In cell lines that overexpress EGF-R or c-erbB-2, it inhibits cell proliferation (IC50, 31 nM) primarily in a cytostatic manner.
Kinase Assay	Liquid scintillation
Kinase Assay	Stock solutions of 500 μM CL-387785 (EKI-785) (prepared in 100% DMSO) are diluted to the desired concentration with 30 mM HEPES, pH 7.4. Ten microlitres of this compound 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.
In vivo	CL-387785 (EKI-785) profoundly blocks the growth of tumour in nude mice overexpressed EGF-R at a dose of 80 mg/kg/day (p.o.). In murine models of autosomal recessive polycystic kidney disease (ARPKD), treatment of Balb/c-bpk/bpk (BPK) mice with this compound (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 it as low as 25 mg/kg reduces the growth of HCA-7-induced xenograft tumour, and a dose of 100 mg/kg prevents tumour growth entirely. A dose of 50 mg/kg is effective at reducing the growth of HCT-116-induced xenograft tumour.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10086326/ [2] https://pubmed.ncbi.nlm.nih.gov/10620185/ [3] https://pubmed.ncbi.nlm.nih.gov/21953075/ [4] https://pubmed.ncbi.nlm.nih.gov/22046346/ [5] https://pubmed.ncbi.nlm.nih.gov/11818567/

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Chemical Structure

Molecular Weight: 381.23