General Information of the Drug (ID: M6APDG03018)
Name
AZD-9496
Synonyms
AZD-9496; AZD-9496 maleate; AZD9496; DA9P7LN909; DFBDRVGWBHBJNR-BBNFHIFMSA-N; (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; (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; 1639042-08-2; CHEMBL3623004; UNII-DA9P7LN909
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Status
Phase 1
Structure
Formula
C25H25F3N2O2
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
InChIKey
DFBDRVGWBHBJNR-BBNFHIFMSA-N
PubChem CID
86287635
INTEDE Drug ID
DR1801
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for AZD-9496. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of AZD-9496 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for AZD-9496. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of AZD-9496 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for AZD-9496. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of AZD-9496 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for AZD-9496. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of AZD-9496 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
References
Ref 1 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 2 Complete Substrate Inhibition of Cytochrome P450 2C8 by AZD9496, an Oral Selective Estrogen Receptor Degrader. Drug Metab Dispos. 2018 Sep;46(9):1268-1276. doi: 10.1124/dmd.118.081539. Epub 2018 Jun 19.