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Src I1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Src I1图片
CAS NO:179248-59-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 373.41
Formula C22H19N3O3
CAS No. 179248-59-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>6 mg/mL
Water: N/A
Ethanol: N/A
Chemical Name6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine
SynonymsSrc I1; SrcI1; Src I-1
SMILES Code

Chemical Name: 6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine

InChi Key: DMWVGXGXHPOEPT-UHFFFAOYSA-N

InChi Code: 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)

SMILES: COC1=CC2=NC=NC(NC3=CC=C(OC4=CC=CC=C4)C=C3)=C2C=C1OC

实验参考方法
In Vitro

In vitro activity: Src Inhibitor 1 ( Src-I1) is a novel, potent and selective dual site Src tyrosine kinase inhibitor which binds competitively to both the ATP- and peptide-binding sites with IC50 values of 44 nM for Src and 88nM for Lck. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency.


Kinase Assay: All assays (25.5 μl volume) were carried out robotically at room temperature (21 °C) and were linear with respect to time and enzyme concentration under the conditions used. Assays were performed for 30 min using Multidrop Micro reagent dispensers (Thermo Electron Corporation, Waltham, MA, U.S.A.) in a 96-well format. The concentration of magnesium acetate in the assays was 10 mM and [γ-33P]ATP (800 c.p.m./pmol) was used at 5, 20 or 50 μM as indicated, in order to be at or below the Km for ATP for each enzyme. Protein kinases assayed at 5 μM ATP were: MKK1, ERK1, p38γ MAPK, p38δ MAPK, ERK8, PKBα, PKCζ, PRK2, GSK3β, CK2, MARK3, IKKβ, DYRK3, PIM2, EF2K, PLK1, Aurora C, HIPK2 and PAK4. Protein kinases assayed at 20 μM ATP were: JNK1, JNK2, p38β MAPK, PDK1, SGK1, S6K1, PKA, ROCK2, PKCα, MSK1, MAPKAP-K2, MAPKAP-K3, PRAK, CaMKKα, CaMKKβ, CHK1, CHK2, CDK2, Aurora B, CK1, PIM1, PIM3, NEK7, MST2, HIPK3, PAK5, PAK6, CSK, Yes and FGF-R1. Protein kinases assayed at 50 μM ATP were: Eph-A2 (Ephrin-A2 receptor), ERK2, JNK3, p38α MAPK, RSK1, RSK2, PKBβ, PKD1, MNK1, MNK2, AMPK, CaMK1, smMLCK, PHK, BRSK2, MELK, DYRK1a, DYRK2, NEK2a, NEK6, SRPK1, Src, Lck, IKKε and TBK1. Protein kinases assayed at 0.1 mM ATP were RIP2, GAK, c-Raf and B-Raf.

In VivoN/A
Animal modelN/A
Formulation & DosageN/A
ReferencesBiochem J. 2007 Dec 15;408(3):297-315; Biochemistry. 2001 Jun 19;40(24):7084-91.