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
| Molecular Formula | C25H25F3N2O2 |
| Molecular Weight | 442.4734 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 1 |
| Optical Activity | UNSPECIFIED |
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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| 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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:44:42 GMT 2023
by
admin
on
Sat Dec 16 08:44:42 GMT 2023
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| Record UNII |
DA9P7LN909
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| Record Status |
Validated (UNII)
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| Record Version |
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C2116
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C122834
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1639042-08-2
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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. |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
Drug: AZD 9496(Primary); Indication: Advanced breast cancer; Focus: Adverse reactions; Sponsor: AstraZeneca; Most Recent Events: 12 Jul 2016 Status changed from recruiting to active, no longer recruiting., 13 May 2016 Planned End Date changed from 1 Sep 2017 to 1 Feb 2018., 13 May 2016 Planned primary completion date changed from 1 Sep 2017 to 1 Feb 2018.
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