Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H25F3N2O2 |
| Molecular Weight | 442.4734 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H]1CC2=C(NC3=C2C=CC=C3)[C@H](N1CC(C)(C)F)C4=C(F)C=C(\C=C\C(O)=O)C=C4F
InChI
InChIKey=DFBDRVGWBHBJNR-BBNFHIFMSA-N
InChI=1S/C25H25F3N2O2/c1-14-10-17-16-6-4-5-7-20(16)29-23(17)24(30(14)13-25(2,3)28)22-18(26)11-15(12-19(22)27)8-9-21(31)32/h4-9,11-12,14,24,29H,10,13H2,1-3H3,(H,31,32)/b9-8+/t14-,24-/m1/s1
AZD 9496 was discovered by AstraZeneca as a potent and selective estrogen receptor downregulator (SERD). This drug participated in phase I clinical trials to evaluate the pharmacokinetic profiles and the safety and tolerability of the different forms, formulations, and doses for the treatment of patients with breast cancer.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist. | 2015 Oct 22 |
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| AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models. | 2016 Jun 1 |
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| Circulating Biomarkers and Resistance to Endocrine Therapy in Metastatic Breast Cancers: Correlative Results from AZD9496 Oral SERD Phase I Trial. | 2018 Dec 1 |
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| The oral selective oestrogen receptor degrader (SERD) AZD9496 is comparable to fulvestrant in antagonising ER and circumventing endocrine resistance. | 2019 Feb |
Sample Use Guides
1.Treatment period 1 will assess AZD9496 Variant A: 100mg.
2.Treatment period 2 will assess AZD9496 Reference: 100mg.
3.Treatment period 3 will assess one of AZD9496 Variants, B, C or D: 100mg.
4.Treatment period 4 will assess one of AZD9496 Variants, B, C or D: 100mg.
Route of Administration:
Oral
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C2116
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AZD-9496
Created by
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PRIMARY | Biological Activity of AZD9496:AZD9496 is a potent and orally bioavailable selective estrogen receptor downregulator(Ki=0.7 nM) and antagonist.IC50 value: 0.7 nM(Ki)0.14 nM(ER downregulation cell IC50)Target: ER downregulatorAZD9496 can induce ER.ALPHA. degradation in breast cancer cell lines at picomolar concentrations. AZD9496 is curently under clinical trials. AZD9496 may be useful for the treatment of ER+ breast cancer. |
ACTIVE MOIETY
