General Information of the Drug (ID: M6APDG02199)
Name
GDC-0032
Synonyms
Taselisib; 1282512-48-4; GDC 0032; UNII-L08J2O299M; 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide; CHEMBL2387080; GDC0032; L08J2O299M; Taselisib [INN]; 2-Methyl-2-(4-{2-[3-Methyl-1-(Propan-2-Yl)-1h-1,2,4-Triazol-5-Yl]-5,6-Dihydroimidazo[1,2-D][1,4]benzoxazepin-9-Yl}-1h-Pyrazol-1-Yl)propanamide; Taselisib [USAN:INN]; GTPL7794; SCHEMBL1485247; SYN1202; DTXSID00155842; BEUQXVWXFDOSAQ-UHFFFAOYSA-N
    Click to Show/Hide
Status
Phase 3
Structure
Formula
C24H28N8O2
InChI
1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
InChIKey
BEUQXVWXFDOSAQ-UHFFFAOYSA-N
PubChem CID
51001932
TTD Drug ID
D0UP1Z
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.
PI3-kinase alpha (PIK3CA)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase alpha (PIK3CA) is a therapeutic target for GDC-0032. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of GDC-0032 through regulating the expression of PI3-kinase alpha (PIK3CA). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase alpha (PIK3CA) is a therapeutic target for GDC-0032. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GDC-0032 through regulating the expression of PI3-kinase alpha (PIK3CA). [2], [3]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary PI3-kinase alpha (PIK3CA) is a therapeutic target for GDC-0032. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of GDC-0032 through regulating the expression of PI3-kinase alpha (PIK3CA). [2], [4]
References
Ref 1 METTL14 Inhibits Hepatocellular Carcinoma Metastasis Through Regulating EGFR/PI3K/AKT Signaling Pathway in an m6A-Dependent Manner. Cancer Manag Res. 2020 Dec 23;12:13173-13184. doi: 10.2147/CMAR.S286275. eCollection 2020.
Ref 2 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44. doi: 10.1038/nrd2926.
Ref 3 Gene signatures and prognostic values of m6A regulators in clear cell renal cell carcinoma - a retrospective study using TCGA database. Aging (Albany NY). 2019 Mar 15;11(6):1633-1647. doi: 10.18632/aging.101856.
Ref 4 ALKBH5 inhibited autophagy of epithelial ovarian cancer through miR-7 and BCL-2. J Exp Clin Cancer Res. 2019 Apr 15;38(1):163. doi: 10.1186/s13046-019-1159-2.