Lasofoxifene

Modify Date: 2024-01-02 18:27:59

Lasofoxifene structure	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	N/A
	MSDS	N/A	Flash Point	300ºC

Use of Lasofoxifene

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].

Name	Lasofoxifene
Synonym	More Synonyms

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/ERR Research Areas >> Cancer Research 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.

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