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 |
|
| AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models. | 2016 Jun 1 |
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
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C2116
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
100000174981
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
PRIMARY | |||
|
C122834
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
PRIMARY | |||
|
1639042-08-2
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
PRIMARY | |||
|
DA9P7LN909
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
PRIMARY | |||
|
86287635
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
PRIMARY | |||
|
DB15138
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
PRIMARY | |||
|
AZD-9496
Created by
admin on Sat Dec 16 08:44:42 GMT 2023 , Edited by admin on Sat Dec 16 08:44:42 GMT 2023
|
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
