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Merck
CN

S2075

Src Inhibitor-1

≥98% (HPLC), Src kinase inhibitor, powder

Synonym(s):

4-(4′-Phenoxyanilino)-6,7-dimethoxyquinazoline, 6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine, SKI-1, Src-l1

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About This Item

Empirical Formula (Hill Notation):
C22H19N3O3
CAS Number:
179248-59-0
Molecular Weight:
373.40
UNSPSC Code:
12352200
PubChem Substance ID:
329824504
NACRES:
NA.77
MDL number:
MFCD01815300

Key Documents

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Product Name

Src Inhibitor-1, ≥98% (HPLC)

SMILES string

COc1cc2ncnc(Nc3ccc(Oc4ccccc4)cc3)c2cc1OC

InChI key

DMWVGXGXHPOEPT-UHFFFAOYSA-N

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)

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: >10 mg/mL

storage temp.

2-8°C

Quality Level

100

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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.

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 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).

Storage Class

11 - Combustible Solids

wgk

WGK 3

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Certificates of Analysis (COA)

Lot/Batch Number
0000505697
0000505696
0000505696
0000505697
0000444146

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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.
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
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
Devin McGee et al.
PloS one, 12(11), e0188645-e0188645 (2017-12-01)
Preterm birth (PTB), or birth before 37 weeks gestation, is the leading cause of neonatal mortality worldwide. Cervical viral infections have been established as risk factors for PTB in women, although the mechanism leading to increased risk is unknown. Using
Scott T Wood et al.
Arthritis & rheumatology (Hoboken, N.J.), 68(1), 117-126 (2015-09-01)
Oxidative posttranslational modifications of intracellular proteins can potentially regulate signaling pathways relevant to cartilage destruction in arthritis. In this study, oxidation of cysteine residues to form sulfenic acid (S-sulfenylation) was examined in osteoarthritic (OA) chondrocytes and investigated in normal chondrocytes
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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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