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CL-387785

Catalog No. T2245 CAS 194423-06-8

Synonyms: WAY-EKI 785, EKI-785

CL-387785 (WAY-EKI 785)(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50： 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a functional level.

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CL-387785, CAS 194423-06-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 178.00
50 mg	In stock	$ 287.00
100 mg	In stock	$ 463.00
500 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 96.68%

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Description	CL-387785 (WAY-EKI 785)(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50： 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a functional level.
Targets&IC50	EGFR:370+/-120 pM
In vitro	CL-387785 demonstrates significant inhibitory effects on the growth of HCT-116-induced xenograft tumors at a dose of 50 mg/kg. In nude mice expressing EGF-R, CL-387785 administered orally at 80 mg/kg/day effectively suppresses tumor growth. In a mouse model of autosomal recessive polycystic kidney disease, treatment with CL-387785 at 90 mg/kg intraperitoneally in Balb/c-bpk/bpk (BPK) mice significantly reduces cystic lesions in collecting ducts, improves kidney function, decreases abnormalities in bile duct epithelial cells, and extends lifespan. At 25 mg/kg, CL-387785 can reduce the growth of HCA-7-induced xenograft tumors, and a dose of 100 mg/kg completely inhibits tumor growth.
In vivo	CL-387785 effectively blocks EGF-mediated receptor autophosphorylation in cells (IC50: 5 nM). It principally acts as a cellular inhibitor, suppressing cell proliferation in cell lines overexpressing EGF-R or c-erbB-2 (IC50: 31 nM).
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 Water 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	MTS assays are performed with the CellTiter 96@ AQueous One solution proliferation kit. A total of 10,000 cells per well in 96-well ?at-bottomed plates are incubated with various concentrations of inhibitors for 48 h. The IC50 is determined from dose–response curves using XL?t4.(Only for Reference)

Synonyms	WAY-EKI 785, EKI-785
Molecular Weight	381.23
Formula	C18H13BrN4O
CAS No.	194423-06-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 59 mg/mL (154.8 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Discafani CM, et al. Biochem Pharmacol. 1999, 57(8), 917-925. 2. William E, et al. Kidney International. 2000, 57(1), 33-40. 3. Hama T, et al. Clin Exp Metastasis. 2012, 29(1), 19-25. 4. Kancha RK, et al. PloS ONE. 2011, 6(10), e26760. 5. Roberts RB, et al. Proc Natl Acad Sci. 2002, 99(3), 1521-1526.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library Anti-Pancreatic Cancer Compound Library Anti-Lung Cancer Compound Library Anti-Colorectal Cancer Compound Library NO PAINS Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CL-387785 194423-06-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR WAY-EKI 785 EKI785 ErbB-1 HER1 CL 387785 WAY-EKI-785 WAY-EKI785 CL387785 inhibit EKI-785 Inhibitor EKI 785 Epidermal growth factor receptor inhibitor

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