| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vitro |
Regardless of the expression levels of activating ERα mutations, lasofoxifene tartrate (1 nM-1 μM; 48 h) exhibits antagonist activity in ER+ breast cancer cells in comparison to wild-type (WT) ERα [2].
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| ln Vivo |
To lessen the severity of arthritis, lasoxifene tartrate (4 mg/mouse; SC; 5 days/week; for 43 days) decreases serum levels of IL-6, an inflammatory cytokine, and cartilage oligomeric matrix protein (COMP), a marker of cartilage degradation [1]. By boosting trabecular bone mineral density (BMD) and cortical thickness in mice, lasoxifene tartrate (4 mg/mouse; subcutaneous injection; 5 days/week; for 43 d) prevents systemic bone loss in CIA [1]. In mice, the subcutaneous injection of lasoxifene tartrate (5 and 10 mg/kg) five days a week for seventy days slows the growth of primary tumors and decreases liver and lung metastases [3].
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| 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
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|---|---|
| Molecular Weight |
413.56
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| Exact Mass |
413.2355
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| CAS # |
190791-29-8
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| Related CAS # |
Lasofoxifene;180916-16-9
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| SMILES |
O(C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])[C@]1([H])C2C([H])=C([H])C(=C([H])C=2C([H])([H])C([H])([H])[C@]1([H])C1C([H])=C([H])C([H])=C([H])C=1[H])O[H].O([H])C([H])(C(=O)O[H])[C@@]([H])(C(=O)O[H])O[H]
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| Synonyms |
CP-336156 Fablyn Lasofoxifene tartrate
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~147.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4180 mL | 12.0901 mL | 24.1803 mL | |
| 5 mM | 0.4836 mL | 2.4180 mL | 4.8361 mL | |
| 10 mM | 0.2418 mL | 1.2090 mL | 2.4180 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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