An orally bioavailable inhibitor of STAT3 (32 and 62% inhibition at 10 and 20 µM

HJC0152 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1420290-99-8
Storage:
-20
UN-No:
De Minimis - 3077 / 9

HJC0152 is an orally bioavailable inhibitor of STAT3 (32 and 62% inhibition at 10 and 20 µM, respectively, in MDA-MB-231 cells in a luciferase reporter assay).{38366} It reduces total STAT3 and phosphorylated STAT3 levels in MDA-MB-231 cells and inhibits nuclear translocation of phosphorylated STAT3. HJC0152 inhibits proliferation of MCF-7 and MDA-MB-231 breast cancer and AsPC-1 and PANC-1 pancreatic cancer cells (IC50s = 0.91, 1.64, 1.9, and 1.08 µM, respectively). It also halts the cell cycle at the G0/G1 phase, induces apoptosis, and suppresses cell proliferation in human head and neck squamous cell carcinoma cells.{38367} HJC0152 (7.5 mg/kg, i.p. or 25 mg/kg, p.o.) inhibits tumor growth in an MDA-MB-231 breast cancer mouse xenograft model and in an orthotopic mouse model of squamous cell carcinoma.{38366,38367}  

 

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Description

An orally bioavailable inhibitor of STAT3 (32 and 62% inhibition at 10 and 20 µM, respectively, in MDA-MB-231 cells in a luciferase reporter assay); inhibits proliferation of MCF-7 and MDA-MB-231 breast cancer and AsPC-1 and PANC-1 pancreatic cancer cells (IC50s = 0.91, 1.64, 1.9, and 1.08 µM, respectively); inhibits tumor growth in a breast cancer mouse xenograft model at doses of 7.5 mg/kg, i.p. or 25 mg/kg, p.o.; inhibits tumor growth in an orthotopic mouse model of squamous cell carcinoma

Formal name: 2-(2-aminoethoxy)-5-chloro-N-(2-chloro-4-nitrophenyl)-benzamide, monohydrochloride

Synonyms: 

Molecular weight: 406.6

CAS: 1420290-99-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Transcription Factors|STATs

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