STAT3-IN-1

Research use only, not for human use.

STAT3-IN-1 selective and orally active inhibitor of STAT3(in HT29 and MDA-MB 231 cells, with IC50 values of 1.82 μM and 2.14 μM , respectively), induces tumor apoptosis.

STAT3-IN-1 selective and orally active inhibitor of STAT3(in HT29 and MDA-MB 231 cells, with IC50 values of 1.82 μM and 2.14 μM , respectively), induces tumor apoptosis. STAT3-IN-1 induces tumor cells apoptosis in MDA-MB-231 cells.

Apoptosis Analysis Cell Line:MDA-MB-231 cell lines.Concentration:0-10 μM.Incubation Time:48 hours.Result:The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%.Western Blot Analysis Cell Line:MDA-MB-231 and HT-29 cell lines.Concentration:0-10 μM.Incubation Time:48 hours.Result:Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685.

Animal Model:Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells.Dosage:10, 20 mg/kg. Administration:Oral administration once every other day for two weeks.Result: Arrested tumor growth with no obvious body weight loss.

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JAK/STAT Signaling

STAT

STAT3

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2059952-75-7

475.53

C28H29NO6

>98% (HPLC)

DMSO:125 mg/mL?(262.86 mM;?Need ultrasonic)

COc1cc(OC)cc(\C=C\c2ccc(NC(=O)\C=C\c3cc(OC)c(OC)c(OC)c3)cc2)c1

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(-20℃)

With Ice Pack

≥ 2 years