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TG100713
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。
TG100713图片
CAS NO:925705-73-3
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)

254.25

Formula

C12H10N6

CAS No.

925705-73-3

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 2 mg/mL (7.86 mM)

Water:<1 mg/mL

Ethanol: <1 mg/mL

Other info

Synonym: TG100713; TG-100713; TG 100713

SMILES Code: OC1=CC=CC(C2=NC3=C(N)N=C(N)N=C3N=C2)=C1

Chemical Name

3-(2,4-diaminopteridin-6-yl)phenol

实验参考方法

In Vitro

Kinase Assay: PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Protein kinase assays are performed by using commercial screening services.

Cell Assay: TG 100713 also strongly inhibits EC proliferation. Human umbilical vein EC (HUVEC) plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF) in the presence or absence of test compounds (10 μM), and cell numbers are quantified by XTT assay.

Modeling studies suggested that the freedom of conformational rotation permitted by ring substituents controls isoform selectivity. Although substituent ring of TG100-115, TG100713, and TG101110 all require energy minima at 30–40°, angles diverge of each compound results in paying differing penalties from this range. TG100-115 displays the greatest barrier to rotation and finally is the most isoform selective, TG100713 has the most conformational flexibility (ring A being almost freely rotatable with maxima ≈5 kcal; 1 kcal = 4.18 kJ), suggesting the least selective, and TG101110 lies an intermediate position (several conformations ≦10 but some>>50 kcal)

In Vivo

The minimum structure which satisfies all three requirements is shown in TG100713, which so far has also displayed the best PI3K binding activity. Interestingly, the SAR profiles generating correlate quite well with the results of the initial in vivo screen further supports the involvement of PI3K as a target for inhibiting vascular permeability in related compounds

Animal model

N/A

Formulation & Dosage

N/A

References

Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71; J Med Chem. 2007 Sep 6;50(18):4279-94.