Bazedoxifene

Research use only, not for human use.

Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively.

Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130.

Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130. Western Blot Analysis Cell Line:AsPC-1 cells Concentration:10 μM, 20 μM Incubation 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:Overnight Result:Induced apoptosis.

Bazedoxifene (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 mice Dosage: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

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198481-32-2

470.6

C30H34N2O3

>98% (HPLC)

DMSO : 100 mg/mL (212.49 mM; Need ultrasonic)

CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=CC=C(O)C=C51

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(-20℃)

With Ice Pack

≥ 2 years