Bazedoxifene acetate

Research use only, not for human use.

Bazedoxifene acetate (TSE 424; WAY-TES 424), a novel selective estrogen receptor modulator (SERM).

Bazedoxifene acetate (TSE 424; WAY-TES 424), a novel selective estrogen receptor modulator (SERM), has been developed to have favorable effects on bone and the lipid profile while minimizing stimulation of uterine or breast tissues. (In Vitro):Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130.(In Vivo):Bazedoxifene acetate (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo.

Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling. Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130. Western Blot Analysis Cell Line:AsPC-1 cells Concentration:10 μM, 20 μMIncubation Time:2 hours Result:Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation. Apoptosis Analysis Cell Line:Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells Concentration:10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC)Incubation Time:Overnigh tResult:Induced apoptosis.

Bazedoxifene acetate (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo. Animal Model:6-week-old female athymic nude miceDosage:5 mg/kg Administration:Oral gavage, daily, for 18 days Result:Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.

TSE 424

Endocrinology/Hormones

Estrogen Receptor/ERR

ERα| ERβ

Cancer

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198481-33-3

530.67

C32H38N2O5

>98% (HPLC)

DMSO: 200 mM

CC1=C(N(CC2=CC=C(OCCN3CCCCCC3)C=C2)C2=C1C=C(O)C=C2)C1=CC=C(O)C=C1

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(-20℃)

With Ice Pack

≥ 2 years