[CAS NO. 194423-06-8]  CL-387785 (EKI-785)

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PRODUCTS SPECIFICATIONS [194423-06-8]

Store
Catalog
SLK-S7557
Brand
Selleck
CAS
194423-06-8

DESCRIPTION [194423-06-8]

Overview

MDLMFCD02179194
Molecular Weight381.23
Molecular FormulaC18H13BrN4O
SMILESN(C=1C2=C(C=CC(NC(C#CC)=O)=C2)N=CN1)C3=CC(Br)=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.6231 mL13.1154 mL26.2309 mL
5 mM0.5246 mL2.6231 mL5.2462 mL
10 mM0.2623 mL1.3115 mL2.6231 mL
50 mM0.0525 mL0.2623 mL0.5246 mL

Description

CL-387785 (EKI-785, WAY-EKI 785) is an irreversible, and selective inhibitor with of 370 pM.

Targets

EGFR [1]
370 pM

In vitro

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.


Synonyms

2-Butynamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-
N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide
CL 387785
EKI 785
WAY-EKI 785
EKB 785