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Palazestrant
- OP1250
- Optical Purity: 100% d.e.
- Soluble in 0.1N HCl(aq), DMSO and EtOH
- MF: C28H36FN3O
- MW: 449.6
Description
Palazestrant is an orally bioavailable complete ER antagonist and selective ER degrader with an IC50 value of 6.4 nM (inhibition of E2 activity). Moreover, Palazestrant demonstrates antiproliferative activity in ER+ breast cancer models that is comparable or superior to other agents of interest.
More Information
| Parent CAS No. | 2092925-89-6 |
|---|---|
| Chemical Name | (1R,3R)-2-(2-Fluoro-2-methylpropyl)-3-methyl-1-(4-(1-propyl-3-azetidinyloxy)phenyl)-2,3,4,9-tetrahydro-1H-β-carboline |
| SMILES | N1C2[C@@H](C3=CC=C(OC4CN(CCC)C4)C=C3)N(CC(F)(C)C)[C@H](C)CC=2C2=CC=CC=C12 |&1:2,23,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C28H36FN3O/c1-5-14-31-16-22(17-31)33-21-12-10-20(11-13-21)27-26-24(23-8-6-7-9-25(23)30-26)15-19(2)32(27)18-28(3,4)29/h6-13,19,22,27,30H,5,14-18H2,1-4H3/t19-,27-/m1/s1 |
| InChiKey | LBSFUBLFDCAEKV-XHCCPWGMSA-N |
| CID | 135351887 |
| Short Description | ER antagonist/degrader |
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