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HS-173
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。
HS-173图片
CAS NO:1276110-06-5
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)

422.46

Formula

C21H18N4O4S

CAS No.

1276110-06-5

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 84 mg/mL warming (198.8 mM)

Water:<1 mg/mL

Ethanol: <1 mg/mL

Other info

Synonym: HS173; HS 173; HS-173.

InChi Key: SEKOTFCHZNXZMM-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H18N4O4S/c1-2-29-21(26)19-13-23-20-9-8-15(14-25(19)20)16-10-17(12-22-11-16)24-30(27,28)18-6-4-3-5-7-18/h3-14,24H,2H2,1H3

SMILES Code: O=C(C1=CN=C2C=CC(C3=CC(NS(=O)(C4=CC=CC=C4)=O)=CN=C3)=CN21)OCC

Chemical Name

Ethyl 6-(5-(phenylsulfonamido)pyridin-3-yl)imidazo[1,2-a]pyridine-3-carboxylate

实验参考方法

In Vitro

Kinase Assay: The PI3K assay is performed using the Kinase-Glo Max luminescent kinase assay kit which quantifies the amount of ADP produced by the PI3K reaction. In brief, an active PI3K (100 ng) is preincubated with compound for 5 min in kinase reaction buffer (25 mM MOPS [pH 7.0], 5 mM MgCl2, and 1 mM EGTA) and 10 μg l-α-phosphatidylinositol (PI). Before addition of PI, it is sonicated with sonication buffer (25 mM MOPS [pH 7.0], 1 mM EGTA) in water for 20 min for allowing miscelle formation. Then reaction is started by the addition of 10 μM ATP and ran for 180 min. To terminate kinase reaction, same volume of Kinase-Glo Max buffer is added. After 10 min, the plates are then read on a GloMax plate reader for luminescence detection.

Cell Assay: Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated with either DMSO as a control or various concentrations of inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. The plate is then read on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose–response curves. To assess the effect of compounds on cell proliferation, T47D cells are cultured with compound (0.1–100 μM) for 48 h before MTT analysis.

HS-173 diminishes blood vessel formation in mice. HS-173 markedly attenuates the development of liver fibrosis by blocking PI3K/Akt signaling in vivo..

In Vivo

Combination of Quercetin (75 mg/kg) and 2-Methoxyestradiol enhances inhibition of human prostate cancer LNCaP and PC-3 cells xenograft tumor growth. LD50:>3000mg/kg (i.g.)

Animal model

Male BALB/c mice with CCl4-induced liver fibrosis

Formulation & Dosage

Dissolved in DMSO, and then mixture (DMSO:PEG400:D.W. = 1:5:4); 20 mg/kg; Oral gavage

References

[1] Kim O, et al. J Med Chem. 2011, 54(7), 2455-2466.; [2] Son MK, et al. Sci Rep. 2013, 3, 3470.

生物活性


Effects of HS-173 on the proliferation of hepatic stellate cells. Sci Rep. 2013, 3, 3470.


Effect of HS-173 on PI3K/AKT signaling in HSC cells.



Effect of HS-173 on CCl4-induced liver fibrosis in mice.