Lasofoxifene
Based on 6 publication(s) in Google Scholar
Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis.
For research use only. We do not sell to patients.
- Purity: 99.27%
- CAS No.: 180916-16-9
- Formula: C28H31NO2
- Molecular Weight:413.55
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Lasofoxifene
More
Biological Activity
Target: Estrogen Receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
13 nM
Compound: 4
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Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells
Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells
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[PMID: 15658851] |
| HeLa | IC50 |
24 nM
Compound: 4
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Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay
Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor beta; ERE assay
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[PMID: 15658851] |
| HeLa | IC50 |
3.1 nM
Compound: 4
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Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay
Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay
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[PMID: 15658851] |
| HeLa | IC50 |
4 nM
Compound: 4
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Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells
Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells
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[PMID: 15658851] |
| MCF7 | IC50 |
0.1 nM
Compound: 4
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Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol
Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol
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[PMID: 16203138] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated)[1]
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Dosage:4 mg/mouse/day
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Administration:Subcutaneous injection; 5 days a week from the first signs of arthritis (day 18); 43 days
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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.
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Animal Model:NSG mices with xenograft tumors model (MIND, mammary intraductal): WT, Y537S and D538G ERα render tumors[3]
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Dosage:1, 5, or 10 mg/kg
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Administration:Subcutaneous injection; 5 days per week; for 70 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 180916-16-9
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Appearance Solid
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Molecular Weight 413.55
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Formula C28H31NO2
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Color White to off-white
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SMILES
OC1=CC=C2[C@@H](C3=CC=C(OCCN4CCCC4)C=C3)[C@@H](C5=CC=CC=C5)CCC2=C1
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Synonyms
CP-336156
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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NPJ Breast Cancer
Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries. [Abstract]2025 Nov 12;11(1):125. PMID: 41224743 -
NPJ Breast Cancer
Unconventional isoquinoline-based SERMs elicit fulvestrant-like transcriptional programs in ER+ breast cancer cells. [Abstract]2022 Dec 14;8(1):130. PMID: 36517522 -
Mol Cancer Ther
The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. [Abstract]2020 Jul;19(7):1395-1405. PMID: 32381587 -
Gynecol Oncol
Constitutively active ESR1 mutations in gynecologic malignancies and clinical response to estrogen-receptor directed therapies. [Abstract]2019 Jul;154(1):199-206. PMID: 30987772 -
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bioRxiv
Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer Cells. [Abstract]2024 Jun 2:2024.05.28.596307. PMID: 38854123
Solvent & Solubility
DMSO : 9.09 mg/mL (21.98 mM; ultrasonic and adjust pH to 4 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.82 mg/mL (4.40 mM); Clear solution
This protocol yields a clear solution of ≥ 1.82 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.82 mg/mL (4.40 mM); Clear solution
This protocol yields a clear solution of ≥ 1.82 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4181 mL | 12.0904 mL | 24.1809 mL | 60.4522 mL |
| 5 mM | 0.4836 mL | 2.4181 mL | 4.8362 mL | 12.0904 mL | |
| 10 mM | 0.2418 mL | 1.2090 mL | 2.4181 mL | 6.0452 mL | |
| 15 mM | 0.1612 mL | 0.8060 mL | 1.6121 mL | 4.0301 mL | |
| 20 mM | 0.1209 mL | 0.6045 mL | 1.2090 mL | 3.0226 mL |
Lasofoxifene Related Classifications
HY-A0037 Related Classifications
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