CAS 180916-16-9|Lasofoxifene
Introduction：Basic information about CAS 180916-16-9|Lasofoxifene, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Lasofoxifene | ||
|---|---|---|---|
| CAS Number | 180916-16-9 | Molecular Weight | 413.55100 |
| Density | 1.15g/cm3 | Boiling Point | 572.4ºC at 760mmHg |
| Molecular Formula | C28H31NO2 | Melting Point | / |
| MSDS | / | Flash Point | 300ºC |
Names
| Name | Lasofoxifene |
|---|---|
| Synonym | More Synonyms |
Lasofoxifene BiologicalActivity
| Description | 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[1][2]. |
|---|---|
| Related Catalog | Signaling Pathways >>Others >>Estrogen Receptor/ERRResearch Areas >>CancerResearch Areas >>Inflammation/Immunology |
| Target | Target: Estrogen Receptor[1] |
| 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]. |
| 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. |
| 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. |
Chemical & Physical Properties
| Density | 1.15g/cm3 |
|---|---|
| Boiling Point | 572.4ºC at 760mmHg |
| Molecular Formula | C28H31NO2 |
| Molecular Weight | 413.55100 |
| Flash Point | 300ºC |
| Exact Mass | 413.23500 |
| PSA | 32.70000 |
| LogP | 5.66660 |
| Vapour Pressure | 1.05E-13mmHg at 25°C |
| Index of Refraction | 1.613 |
| InChIKey | GXESHMAMLJKROZ-IAPPQJPRSA-N |
| SMILES | Oc1ccc2c(c1)CCC(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 |
Synonyms
| lasofoxifen |
| CP-336,156 |
