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S2075

Sigma-Aldrich

Src Inhibitor-1

≥98% (HPLC)

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Synonym(s):
4-(4′-Phenoxyanilino)-6,7-dimethoxyquinazoline, 6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine, SKI-1, Src-l1
Empirical Formula (Hill Notation):
C22H19N3O3
CAS Number:
179248-59-0
Molecular Weight:
373.40
MDL number:
MFCD01815300
UNSPSC Code:
12352200
PubChem Substance ID:
329824504
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: >10 mg/mL

storage temp.

2-8°C

SMILES string

COc1cc2ncnc(Nc3ccc(Oc4ccccc4)cc3)c2cc1OC

InChI

1S/C22H19N3O3/c1-26-20-12-18-19(13-21(20)27-2)23-14-24-22(18)25-15-8-10-17(11-9-15)28-16-6-4-3-5-7-16/h3-14H,1-2H3,(H,23,24,25)

InChI key

DMWVGXGXHPOEPT-UHFFFAOYSA-N

Application

Src Inhibitor-1 may be used in Src kinase-mediated cell signaling studies.

Biochem/physiol Actions

Apart from Src kinase, some Src inhibitors also inhibit the activity of Abl kinase, Lck, Csk and Yes proteins and are therefore being explored as viable anti-cancer drug options.
Src Inhibitor-1 is a potent, competitve dual site (both the ATP- and peptide-binding) Src kinase inhibitor. Src Inhibitor-1 is one of the "gold standards" for Src kinase inhibition. It has been shown to use PP1 or PP2 in parallel with Src-I1 to inhbit Src family kinases. Src Inhibitor-1 is a selective, competitive inhibitor of Src family of tyrosine kinases (IC50 = 44 nM and 88 nM for Src and Lck, respectively). Src Inhibitor-1 Inhibits VEGFR2 and c-fms tyrosine kinases at much higher concentrations (IC50 = 0.32 μM and 30 μM, respectively).

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

WGK

WGK 3

Certificates of Analysis (COA)

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Diane H Boschelli et al.
Journal of medicinal chemistry, 47(7), 1599-1601 (2004-03-19)
We previously reported that several 7-alkoxy-4-phenylamino-3-quinolinecarbonitriles were potent inhibitors of Src kinase activity. We disclose here a new highly efficient and versatile route to these compounds, which are also potent inhibitors of Abl kinase.
Klaske M Schukken et al.
Life science alliance, 3(2) (2020-01-26)
Chromosomal instability (CIN) and aneuploidy are hallmarks of cancer. As most cancers are aneuploid, targeting aneuploidy or CIN may be an effective way to target a broad spectrum of cancers. Here, we perform two small molecule compound screens to identify
Lei Chen et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 57, 72-83 (2019-01-23)
Periploca forrestii(PF) is mainly utilized for treatment of arthritis and traumatic injury historically. We had previously demonstrated that a fraction rich in cardiotonic steroids isolated from PF had the potential to facilitate wound healing. However, the exact material basis and
Yi-Fang Yang et al.
Oncogenesis, 9(8), 78-78 (2020-08-31)
Cholesterol is the major component of lipid rafts. Squalene synthase (SQS) is a cholesterol biosynthase that functions in cholesterol biosynthesis, modulates the formation of lipids rafts and promotes lung cancer metastasis. In this study, we investigated the lipid raft-associated pathway
Thomas Nerreter et al.
Experimental hematology, 42(9), 773-782 (2014-06-03)
The SRC family of kinases (SFKs) is crucial to malignant growth, but also important for signaling in immune cells such as dendritic cells (DCs). These specialized antigen-presenting cells are essential for inducing and boosting specific T-cell responses against pathogens and
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Articles

Src Family Kinases Overview

Src is the original member of a group of non-receptor protein-tyrosine kinases termed the Src family kinases (SFKs). Learn about the SFKs that, in humans, consist of eight members, a small group of atypical members, and two related kinases.

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