Lasofoxifene (tartrate)

Chemical Information
Lasofoxifene Tartrate is the tartrate salt form of lasofoxifene, a non-steroidal, naphthalene-derived, third-generation selective estrogen receptor modulator (SERM) with potential antineoplastic and anti-osteoporotic activities. Upon oral administration, lasofoxifene selectively binds to both estrogen receptor alpha (ERalpha; ESR1) and estrogen receptor beta (ERbeta; ESR2) with high affinity and mimics the effects of endogenous estradiol with varying agonist and antagonist effects in ER-expressing tissues. Blockade of ERalpha by lasofoxifene may potentially inhibit estrogen-dependent cancer cell proliferation in ER-expressing cancers. Lasofoxifene may also bind to the certain mutant forms of ERalpha, including the Y537S ESR1 mutant, making it potentially useful in the treatment of tumors that have acquired resistance to other ER-targeting agents.
| CAS Number | 190791-29-8 |
| PubChem CID | 3081919 |
| IUPAC Name | (2S,3S)-2,3-dihydroxybutanedioic acid;(5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol |
| Molecular Formula | C32H37NO8 |
| Molecular Weight | 563.6 |
| Topological Polar Surface Area | 148 |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 9 |
| Heavy Atom Count | 41 |
| Formal Charge | 0 |
| Complexity | 667 |
| Property | Value |
|---|---|
| Molecular Weight | 563.6 |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 9 |
| Rotatable Bond Count | 9 |
| Exact Mass | 563.25191714 |
| Monoisotopic Mass | 563.25191714 |
| Topological Polar Surface Area | 148 Ų |
| Heavy Atom Count | 41 |
| Formal Charge | 0 |
| Complexity | 667 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 4 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 2 |
| Compound Is Canonicalized | Yes |
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