CL-387785 (Synonyms: EKI-785; WAY-EKI 785)

Name: CL-387785
Brand: MedChemExpress
SKU: HY-10325
Rating: 5.0 (2 reviews)

Cat. No.: HY-10325 Purity: 99.11%: Data Sheet
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CL-387785 (EKI-785; WAY-EKI 785) is an orally active EGFR inhibitor with an IC₅₀ of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC₅₀ of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.

For research use only. We do not sell to patients.

CL-387785 Chemical Structure

CAS No. : 194423-06-8

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of CL-387785:

CL-387785 (Standard) Get quote

2 Publications Citing Use of MCE CL-387785

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR

370 pM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.079 μM Compound: 1	Inhibition of cell growth of human epidermoid carcinoma xenograft (A431) model using cell based assay Inhibition of cell growth of human epidermoid carcinoma xenograft (A431) model using cell based assay	[PMID: 11495584]
A-431	IC₅₀	5 nM Compound: 14, CL-387785	Inhibition of EGF-induced autophosphorylation of EGFR in human A431 cells Inhibition of EGF-induced autophosphorylation of EGFR in human A431 cells	[PMID: 22621397]
BaF3	IC₅₀	1.06 μM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2 nM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2 nM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2.69 μM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	2.81 μM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR A767_V769dupASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR A767_V769dupASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	26 nM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring wildtype ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring wildtype ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	3.17 μM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	4 nM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	75 nM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins 774YVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins 774YVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	8 nM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins G776V,C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring ERBB2 Ins G776V,C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
BaF3	IC₅₀	> 3.3 μM Compound: CL-387,785	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
Calu-3	IC₅₀	100 nM Compound: CL-387,785	Antiproliferative activity against human Calu-3 cells harboring ERBB2 amp mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Calu-3 cells harboring ERBB2 amp mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
HCC827	IC₅₀	2 nM Compound: CL-387,785	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NCI-H1975	IC₅₀	850 nM Compound: CL-387,785	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NCI-H3255	IC₅₀	23 nM Compound: CL-387,785	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
NIH3T3	IC₅₀	2.5 nM Compound: 20	Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells	[PMID: 16480284]
PC-9	IC₅₀	2 nM Compound: CL-387,785	Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 20033049]
SK-BR-3	IC₅₀	0.017 μM Compound: 1	Inhibition of cell growth of SKBr3 cell lines using cell-based assay Inhibition of cell growth of SKBr3 cell lines using cell-based assay	[PMID: 11495584]
SW-620	IC₅₀	1.5 μM Compound: 1	Inhibition of cell growth of SW620 cell lines using cell-based assay Inhibition of cell growth of SW620 cell lines using cell-based assay	[PMID: 11495584]
Sf9	IC₅₀	0.2 μM Compound: EKI-785	TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells	[PMID: 15155841]

In Vitro

CL-387,785 (30-1000 nM; 3 days) induces G0/G1 cell cycle arrest in A431 and SK-BR-3 cells at concentrations of 300-1000 nM after 3 days of incubation, with minimal apoptosis at higher doses^[2].
CL-387,785 (0.1-30 μM; 48 h) inhibits the growth of gefitinib-resistant Ba/F3-EGFR^L858R-T790M cells with a cellular IC₅₀ of ~1 μmol/L^[3].
CL-387,785 (3 μM; 24 h) induces significant apoptosis in gefitinib-resistant Ba/F3-EGFR^L858R-T790M cells and sensitive Ba/F3-EGFR^L858R cells^[3].
CL-387,785 (0.3-10 μM; 6 h) inhibits phosphorylation of EGFR and its downstream signaling targets STAT5, AKT, and ERK 1/2 in gefitinib-resistant Ba/F3-EGFR^L858R-T790M cells with an IC₅₀ of ~1 μmol/L^[3].
CL-387,785 (0.1-3 μM; 6 h) completely inhibits phosphorylation of EGFR and its downstream signaling targets STAT5, AKT, and ERK 1/2 in gefitinib-resistant H1975 lung cancer cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[2]

Cell Line:	A431 cells; SK-BR-3 cells
Concentration:	30, 300, 1000 nM
Incubation Time:	3 days
Result:	Increased the percentage of A431 cells in G0/G1 phase to 73% from 56% in untreated controls, with corresponding decreases in S phase (16% vs 28%) and G2/M phase (8% vs 15%) at 300 nM. Increased SK-BR-3 cells in G0/G1 phase to 82% and 84%, respectively, from 63% in controls, with S phase reduced to 4% and 4%, and G2/M phase reduced to 3% and 3% at 300 nM and 1000 nM. Induced 7% apoptotic cells in A431 cells at 1000 nM, and 10-11% apoptotic cells in SK-BR-3 cells at 300-1000 nM.

Apoptosis Analysis^[3]

Cell Line:	Ba/F3-L858R, Ba/F3-L858R-T790M stable cell lines
Concentration:	3 μM
Incubation Time:	24 h
Result:	Induced high levels of apoptosis in both Ba/F3-L858R and gefitinib-resistant Ba/F3-L858R-T790M cells, with apoptosis rates comparable to those induced by gefitinib in Ba/F3-L858R cells.

Western Blot Analysis^[3]

Cell Line:	Ba/F3-L858R, Ba/F3-L858R-T790M stable cell lines
Concentration:	0.3, 1, 3 and 10 μM
Incubation Time:	6 h
Result:	Potently inhibited phosphorylation of EGFR, STAT5, AKT, and ERK 1/2 in both Ba/F3-L858R and gefitinib-resistant Ba/F3-L858R-T790M cells, with an IC₅₀ of ~1 μM for inhibition of all examined phosphorylated proteins in Ba/F3-L858R-T790M cells.

Apoptosis Analysis^[3]

Cell Line:	H1975 (lung adenocarcinoma, EGFR L858R-T790M mutant) cell line
Concentration:	1 μM
Incubation Time:	48 h
Result:	Induced a mean apoptotic cell percentage of 42.1% in H1975 cells, a statistically significant increase compared to control (8.84%) and gefitinib-treated (8.73%) cells.

Western Blot Analysis^[3]

Cell Line:	H1975 (lung adenocarcinoma, EGFR L858R-T790M mutant) cell line
Concentration:	0.3, 1, 3 and 10 μM
Incubation Time:	6 h
Result:	Completely inhibited phosphorylation of EGFR, STAT5, AKT, and ERK 1/2 in H1975 cells at 1 μM.

In Vivo

CL-387785 (25-100 mg/kg; intraperitoneal injection; once every 3 days; days 18-46) dose-dependently reduces collecting duct cyst formation, improves renal function, attenuates biliary abnormalities, and prolongs survival in autosomal recessive polycystic kidney disease mice^[1].
CL-387785 (20-80 mg/kg; i.p., p.o.; intermittent administration with repeated dosing for 10 consecutive days) inhibits the growth of EGF-R-overexpressing A431 tumors in nude mice, and the tumors respond to the repeated dosing regimen^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Balb/c-bpk/bpk (postnatal)^[1]
Dosage:	25 mg/kg; 50 mg/kg; 60 mg/kg; 80 mg/kg; 90 mg/kg (short-term and long-term survival studies); 100 mg/kg
Administration:	i.p.; every 3 days; 6 total doses (short-term); every 3 days from postnatal day 7 to postnatal day 46 (long-term survival)
Result:	Effectively alleviated the cyst growth and bile duct lesions in the ARPKD model mice, improved renal function, and significantly prolonged their lifespan.

Animal Model:	Athymic nu/nu (female)^[2]
Dosage:	80 mg/kg (i.p., intermittent schedule); 20 mg/kg (i.p., daily x10 days, repeated); 80 mg/kg (p.o., daily x10 days, repeated)
Administration:	i.p. (days 1, 5, 9, 21, 25, 29); i.p. (daily on days 1 through 10 and days 21 through 30); p.o. (daily on days 1 through 10 and days 21 through 30)
Result:	Produced significant tumor growth inhibition. Showed tumor regrowth after initial 10-day treatment course, but tumors responded to a second 10-day treatment course.

Molecular Weight

381.23

Formula

C₁₈H₁₃BrN₄O

CAS No.

194423-06-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)C#CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (262.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6231 mL	13.1154 mL	26.2309 mL
5 mM	0.5246 mL	2.6231 mL	5.2462 mL
10 mM	0.2623 mL	1.3115 mL	2.6231 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.11%

Select Batch:

Data Sheet (292 KB) SDS (644 KB)

COA (247 KB) HNMR (143 KB) RP-HPLC (264 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57(1):33-40.
[Content Brief]

[2]. Discafani CM, et al. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785). Biochem Pharmacol. 1999;57(8):917-925. [Content Brief]

[3]. Kobayashi S, et al. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res. 2005 Aug 15;65(16):7096-101.
[Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6231 mL	13.1154 mL	26.2309 mL	65.5772 mL
	5 mM	0.5246 mL	2.6231 mL	5.2462 mL	13.1154 mL
	10 mM	0.2623 mL	1.3115 mL	2.6231 mL	6.5577 mL
	15 mM	0.1749 mL	0.8744 mL	1.7487 mL	4.3718 mL
	20 mM	0.1312 mL	0.6558 mL	1.3115 mL	3.2789 mL
	25 mM	0.1049 mL	0.5246 mL	1.0492 mL	2.6231 mL
	30 mM	0.0874 mL	0.4372 mL	0.8744 mL	2.1859 mL
	40 mM	0.0656 mL	0.3279 mL	0.6558 mL	1.6394 mL
	50 mM	0.0525 mL	0.2623 mL	0.5246 mL	1.3115 mL
	60 mM	0.0437 mL	0.2186 mL	0.4372 mL	1.0930 mL
	80 mM	0.0328 mL	0.1639 mL	0.3279 mL	0.8197 mL
	100 mM	0.0262 mL	0.1312 mL	0.2623 mL	0.6558 mL

CL-387785 Related Classifications

Help & FAQs

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CL-387785 (Synonyms: EKI-785; WAY-EKI 785)

Customer Review

Other Forms of CL-387785:

2 Publications Citing Use of MCE CL-387785

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

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References

Customer Review

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Complete Stock Solution Preparation Table

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CL-387785 (Synonyms: EKI-785; WAY-EKI 785)

Customer Review

Other Forms of CL-387785:

CL-387785 Related Antibodies

2 Publications Citing Use of MCE CL-387785

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

CL-387785 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CL-387785 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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