Lasofoxifene (CP-336156) 是一种具有口服活性和选择性的雌激素受体调节剂 (SERM)。Lasofoxifene 具有抗骨质疏松的功能，还能抑制原生肿瘤生长和转移。Lasofoxifene 可用于乳腺癌和绝经后骨质疏松症的研究。
| 生物活性 | Lasofoxifene (CP-336156) is an orally active and selectiveestrogen receptormodulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breastcancerand postmenopausal osteoporosis[1][2]. |
| IC50& Target | Target: Estrogen Receptor[1] |
体外研究
(In Vitro) | Lasofoxifene (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[2].
|
体内研究
(In Vivo) | Lasofoxifene (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 in mice[1].
Lasofoxifene (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[1].
Lasofoxifene (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[3].
| Animal Model: | Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated)[1] | | 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[3] | | 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. |
|
| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com