| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| 250mg |
| ln Vitro |
Regardless of the expression levels of activating ERα mutations, lasoxifene (1 nM-1 μM; 48 hours) exhibits antagonist activity in ER+ breast cancer cells in comparison to wild-type (WT) ERα [2].
|
|---|---|
| ln Vivo |
Lasoxifene (4 mg/mouse; subcutaneous injection; 5 days/week; for 43 days) by reducing cartilage oligomeric matrix protein (COMP), a serum marker of cartilage destruction, and lowering serum IL-6, an inflammatory Cytokines) levels, reducing the severity of arthritis in mice [1]. Lasoxifene (4 mg/mouse; subcutaneous injection; 5 days/week; for 43 d) prevents systemic bone loss in CIA by increasing trabecular bone mineral density (BMD) and cortical thickness in mice [1] . Lasoxifene (5 and 10 mg/kg; subcutaneous injection; 5 days/week; for 70 days) inhibits primary tumor growth and reduces lung and liver metastasis in mice [3].
|
| Animal Protocol |
Animal/Disease Models: OVX (ovariectomized) DBA/1 mouse postmenopausal RA model (female DBA/1 mice, 8-10 weeks old, CIA treated) [1]
Doses: 4 mg/mouse/day Route of Administration: subcutaneous injection; 5 days per week from first signs of arthritis (Day 18); 43 days Experimental Results: Reduction in arthritis severity, including reduction in synovial inflammation and joint destruction. At 42 days post-immunization, the average incidence of arthritis was 47% compared with 81% in the vehicle group. Animal/Disease Models: NSG Mouse xenograft tumor model (MIND, mammary intraductal): WT, Y537S and D538G ERα renders tumors [3] Doses: 1, 5 or 10 mg/kg Route of Administration: SC; 5 days per week ; 70-day Experimental Results: Excellent inhibitory effect at 10 mg/kg, resulting in potential tumor shrinkage of Y537S and D538G tumors. At doses of 5 mg/kg and 10 mg/kg, tumor weight was diminished to 60% and 50% for Y537S and D538G, respectively. |
| References |
[1]. Andersson A, et al. Selective oestrogen receptor modulators lasofoxifene and bazedoxifene inhibit joint inflammation and osteoporosis in ovariectomised mice with collagen-induced arthritis. Rheumatology (Oxford). 2016 Mar;55(3):553-63.
[2]. Andreano KJ, et al. The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. Mol Cancer Ther. 2020 Jul. 19(7):1395-1405. [3]. Lainé M, et al. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Breast Cancer Res. 2021 May 12. 23(1):54. |
| Molecular Formula |
C28H31NO2
|
|---|---|
| Molecular Weight |
413.55
|
| Exact Mass |
413.23548
|
| CAS # |
180916-16-9
|
| Related CAS # |
Lasofoxifene tartrate;190791-29-8
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
C1=CC=C(C=C1)[C@H]2CCC3=CC(=CC=C3[C@H]2C4=CC=C(C=C4)OCCN5CCCC5)O
|
| Synonyms |
CP 336156; CP 336,156; Lasofoxifene; CP336,156; CP336156; CP-336156; CP-33,6156; trade name Fably; Oporia;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4181 mL | 12.0904 mL | 24.1809 mL | |
| 5 mM | 0.4836 mL | 2.4181 mL | 4.8362 mL | |
| 10 mM | 0.2418 mL | 1.2090 mL | 2.4181 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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