Lasofoxifene (CP-336156) tartrate 是一种具有口服活性和选择性的雌激素受体调节剂 (SERM)。Lasofoxifene tartrate 具有抗骨质疏松的功能，还能抑制原生肿瘤生长和转移。Lasofoxifene tartrate 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) tartrate is an orally active and selectiveestrogen receptormodulator (SERM)[1]. Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breastcancerand postmenopausal osteoporosis[1][2]. |
| IC50& Target | Target: Estrogen Receptor[1] |
体外研究
(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[2].
|
体内研究
(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[1].
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[1].
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[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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(147.84 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL | | 5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | | 10 mM | 0.1774 mL | 0.8871 mL | 1.7742 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.69 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.69 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com