[CAS NO. 1420290-99-8] HJC0152

Name: HJC0152
Brand: Arctom Scientific
SKU: SLK-S8561

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PRODUCTS SPECIFICATIONS [1420290-99-8]

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Catalog

SLK-S8561

Brand

Selleck

CAS

1420290-99-8

DESCRIPTION [1420290-99-8]

Overview

MDL	MFCD29770804
Molecular Weight	406.65
Molecular Formula	C15H13Cl2N3O4.HCl
SMILES	O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.4591 mL	12.2956 mL	24.5912 mL
5 mM	0.4918 mL	2.4591 mL	4.9182 mL
10 mM	0.2459 mL	1.2296 mL	2.4591 mL
50 mM	0.0492 mL	0.2459 mL	0.4918 mL

Description

HJC0152 is a inhibitor with remarkably improved aqueous solubility.

Targets

STAT3 ^[1]

In vitro

HJC0152 inhibits STAT3 promoter activity in MDA-MB-231 cells in a dose-dependent manner. It has a comparable potency in downregulating STAT3 protein production and phosphorylation at the Tyr-705 site. HJC0152 induces cleaved caspase-3 and downregulated cyclin D1 in MDA-MB-231 cells, inhibits cell cycle progression and promotes apoptosis. HJC0152 treatment efficiently suppresses HNSCC cell proliferation, arrests the cell cycle at the G0/G1 phase, induces apoptosis, and reduced cell invasion in both SCC25 and CAL27 cell lines. Moreover, HJC0152 inhibits nuclear translocation of phosphorylated STAT3 at Tyr705 and decreases VHL/β-catenin signaling activity via regulation of microRNA-21.

In vivo

HJC0152 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo (ip and po), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancer. It has an improved oral bioavailability and an enhanced suppression of tumor growth in mice. HJC0152 does not show significant signs of toxicity at a dose of 75 mg/kg. In SCC25-derived orthotopic mouse models, HJC0152 treatment significantly abrogates STAT3/β-catenin expression in vivo, which leading to a global decrease of tumor growth and invasion.

References

[1] Chen H, et al. ACS Med Chem Lett. 2013, 4(2):180-185.
[2] Wang Y, et al. Mol Cancer Ther. 2017, 16(4):578-590.