Lasofoxifene Tartrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

酒石酸拉索昔芬是第三代非甾体选择性雌激素受体调节剂。

Lasofoxifene Tartrate?is a third-generation non-steroidal selective estrogen receptor modulator.(In Vitro):Lasofoxifene tartrate (1 nM-1 μM; 48 h) shows antagonist activity on ER+ breast cancer cells without being affected by the expression level of activating ERα mutants relative to wild-type (WT) ERα.(In Vivo):Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels.Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice.Lasofoxifene tartrate (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice.

Lasofoxifene tartrate (1 nM-1 μM; 48 h) shows antagonist activity on ER+ breast cancer cells without being affected by the expression level of activating ERα mutants relative to wild-type (WT) ERα.

Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels.Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice.Lasofoxifene tartrate (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice. Animal Model:Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated) Dosage:4 mg/mouse/day Administration:Subcutaneous injection; 5 days a week from the first signs of arthritis (day 18); 43 days Result:Reduced in arthritis severity, including synovial inflammation and destruction of joints reduction.The mean arthritis frequency was 47% while the vehicle group was 81% at 42 days post immunization.Animal Model:NSG mices with xenograft tumors model (MIND, mammary intraductal): WT, Y537S and D538G ERα render tumors Dosage:1, 5, or 10 mg/kg Administration:Subcutaneous injection; 5 days per week; for 70 days Result:Elicited a superior inhibitory effect at a dose of 10 mg/kg, resulted potential tumor shrinkage in Y537S and D538G tumors. And also reduced tumor weight to 60% for Y537S and 50% for D538G at 5 and 10 mg/kg, respectively.

CP-336156

Endocrinology/Hormones

Estrogen Receptor/ERR

oestrogen receptor

Cancer

Locally Advanced or Metastatic Breast Cancer

190791-29-8

563.64

C32H37NO8

>98% (HPLC)

DMSO:6 mg/mL (10.65 mM)

O=C(O)C(O)C(O)C(=O)O.Oc1ccc2c(c1)CCC(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1

(5R6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5678-tetrahydronaphthalen-2-ol

(-20℃)

With Ice Pack

≥ 2 years