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CL-387785 (EKI-785)

Irreversible inhibiter of EGFR CAS# 194423-06-8

CL-387785 (EKI-785)

Catalog No. BCC6436----Order now to get a substantial discount!

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Chemical structure

CL-387785 (EKI-785)

3D structure

Chemical Properties of CL-387785 (EKI-785)

Cas No. 194423-06-8 SDF Download SDF
PubChem ID 2776 Appearance Powder
Formula C18H13BrN4O M.Wt 381.23
Type of Compound N/A Storage Desiccate at -20°C
Synonyms EKI-785; WAY-EKI 785
Solubility DMSO : 13.67 mg/mL (35.86 mM; Need ultrasonic and warming)
Chemical Name N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide
SMILES CC#CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br
Standard InChIKey BTYYWOYVBXILOJ-UHFFFAOYSA-N
Standard InChI InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CL-387785 (EKI-785)

DescriptionCL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. IC50 value: 370+/-120 pM Target: EGFR in vitro: CL-387785 blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2 [1]. Whereas transformation by most EGFR mutants confers on cells sensitivity to erlotinib and gefitinib, transformation by an exon 20 insertion makes cells resistant to these inhibitors but more sensitive to the irreversible inhibitor CL-387,785 [3]. CL-387,785 is able to overcome resistance caused by the T790M mutation on a functional level, correlating with effective inhibition of downstream signaling pathways [4]. in vivo: CL-387785 profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80 mg/kg/day for 10 days, daily) [1]. Treatment of BPK mice with EKI-785 resulted in a marked reduction of collecting tubule (CT) cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and an increased life span. Cystic animals treated with EKI-785 to postnatal day 48 (P-48) were alive and well with normal renal function, a reduced CT cystic index of 2.0 (P < 0.02), a threefold increased in maximum urinary concentrating ability (P < 0.01), and a significant decrease in biliary epithelial proliferation/fibrosis (P < 0.01) [2].

References:
[1]. 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 Apr 15;57(8):917-25. [2]. Sweeney WE, et al. Treatment of polycystic kidney disease with a novel tyrosine kinase inhibitor. Kidney Int. 2000 Jan;57(1):33-40. [3]. Greulich H, et al. Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. PLoS Med. 2005 Nov;2(11):e313. [4]. 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.

CL-387785 (EKI-785) Dilution Calculator

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CL-387785 (EKI-785) Molarity Calculator

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Preparing Stock Solutions of CL-387785 (EKI-785)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6231 mL 13.1154 mL 26.2309 mL 52.4618 mL 65.5772 mL
5 mM 0.5246 mL 2.6231 mL 5.2462 mL 10.4924 mL 13.1154 mL
10 mM 0.2623 mL 1.3115 mL 2.6231 mL 5.2462 mL 6.5577 mL
50 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.0492 mL 1.3115 mL
100 mM 0.0262 mL 0.1312 mL 0.2623 mL 0.5246 mL 0.6558 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CL-387785 (EKI-785)

Description:

IC50: 370 pM

The EGFR is a 170-kDa protein that contains an extracellular ligand binding domain, a single transmembrane domain, and an intracellular tyrosine kinase domain. EGF-R is hyperactivated in numerous tumors including those derived from the lung, brain, bladder, prostate, head, and neck. It has been shown previously that 4-anilino quinazolines compete with the ability of ATP binding the EGFR, inhibit EGF-stimulated autophosphorylation of tyrosine residues in EGFR, and block EGF-mediated growth. CL-387785 is an irreversible inhibiter of EGFR.

In vitro: CL-387785 covalently bound to EGFR. It also specifically inhibited kinase activity of the protein, blocked EGF-stimulated autophosphorylation of the receptor in cells, inhibited cell proliferation primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2 [1].

In vivo: The effects of CL-387785 on tumor growth were assessed in human tumor xenografts implanted s.c. in the flanks of nude mice. CL-387785 inhibited the growth of tumors derived from A431 cells when the drug was administered i.p. or p.o.. Inhibitory effects were observed within 7 days after the onset of therapy. No efficacy was observed with CL-387785 in tumors derived from cell lines that did not overexpress EGF-R, including the human breast carcinoma MDA-MB-435 [1].

Clinical trial: Up to now, CL-387785 is still in the preclinical development stage.

Reference:
[1] Discafani CM, Carroll ML, Floyd MB Jr, Hollander IJ, Husain Z, Johnson BD, Kitchen D, May MK, Malo MS, Minnick AA Jr, Nilakantan R, Shen R, Wang YF, Wissner A, Greenberger LM.  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 Apr 15;57(8):917-25.

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Description

CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.

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