HJC0152|cas 1420290-99-8

Cas No.:	1420290-99-8
SMILES:	OC1=CC(C(NCC(N[C@@H](CC(O)=O)C2=CC(Br)=CC(C(C)(C)C)=C2)=O)=O)=CC(NC3=NCC(CN3)O)=C1
Formula:	C₁₅H₁₃Cl₂N₃O₄^.HCl
M.Wt:	406.65
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC44161	AS1810722	AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722 has the potential for allergic diseases such as asthma and atopic diseases.
DC41884	APTSTAT3-9R	APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
DC41461	Angoline hydrochloride	Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
DC41460	Angoline	Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
DC40121	(R)-Lisofylline	(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 μM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
DC10626	HJC0152	HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
DC10111	Debio 0617B	Debio 0617B has been developed as a first-in-class kinase inhibitor with a unique profile targeting phospho-STAT3 (pSTAT3) and/or pSTAT5 in tumors through combined inhibition of JAK, SRC, ABL, and class III/V receptor tyrosine kinases (RTK).
DC12009	CPA-7	A platinum-containing compound that disrupts STAT3 signaling, inhibits cell growth and induces apoptosis in STAT3-activated cancer cells.
DC11882	HJC0416	A orally bioavailable small-molecule STAT3 inhibitor.
DC12010	ML116	A novel selective STAT3 inhibitor with IC50 of 4.2 uM, does not inhibit STAT1, STAT5, or NFkB signaling pathways (IC50>50 uM).