Lasofoxifene Tartrate

CAS No. 190791-29-8

Lasofoxifene Tartrate( CP-336156 )

Catalog No. M21094 CAS No. 190791-29-8

Lasofoxifene Tartrate?is a third-generation non-steroidal selective estrogen receptor modulator.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Lasofoxifene Tartrate
  • Note
    Research use only, not for human use.
  • Brief Description
    Lasofoxifene Tartrate?is a third-generation non-steroidal selective estrogen receptor modulator.
  • Description
    Lasofoxifene Tartrate?is a third-generation non-steroidal selective estrogen receptor modulator.(In Vitro):Lasofoxifene tartrate (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.(In Vivo):Lasofoxifene tartrate (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.Lasofoxifene tartrate (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.Lasofoxifene tartrate (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.
  • In Vitro
    Lasofoxifene tartrate (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.
  • In Vivo
    Lasofoxifene tartrate (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.Lasofoxifene tartrate (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.Lasofoxifene tartrate (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. Animal Model:Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated) 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 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.
  • Synonyms
    CP-336156
  • Pathway
    Endocrinology/Hormones
  • Target
    Estrogen Receptor/ERR
  • Recptor
    oestrogen receptor
  • Research Area
    Cancer
  • Indication
    Locally Advanced or Metastatic Breast Cancer

Chemical Information

  • CAS Number
    190791-29-8
  • Formula Weight
    563.64
  • Molecular Formula
    C32H37NO8
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:6 mg/mL (10.65 mM)
  • SMILES
    O=C(O)C(O)C(O)C(=O)O.Oc1ccc2c(c1)CCC(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1
  • Chemical Name
    (5R6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5678-tetrahydronaphthalen-2-ol

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Andersson A Bernardi A I Stubelius A et al. Selective oestrogen receptor modulators lasofoxifene and bazedoxifene inhibit joint inflammation and osteoporosis in ovariectomised mice with collagen-induced arthritis[J]. Rheumatology 2015:kev355.
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