General Information of the Drug (ID: M6APDG01102)
Name
ACTB-1003
Synonyms
Multi-mode kinase inhibitor (oral, cancer), ACT Biotech; Multi-mode kinase inhibitor (oral, cancer), Bayer
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Status
Investigative
Structure
Formula
C27H26F5N7O3
InChI
1S/C27H26F5N7O3/c1-41-13-17-22(12-38-6-8-42-9-7-38)39-24(25(33)34-14-35-39)23(17)15-2-5-20(19(29)10-15)36-26(40)37-21-11-16(27(30,31)32)3-4-18(21)28/h2-5,10-11,14H,6-9,12-13H2,1H3,(H2,33,34,35)(H2,36,37,40)
InChIKey
GZPJCJKUZPUFAL-UHFFFAOYSA-N
PubChem CID
23653175
TTD Drug ID
D0R6OM
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.
Fibroblast growth factor receptor 4 (FGFR4)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Fibroblast growth factor receptor 4 (FGFR4) is a therapeutic target for ACTB-1003. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of ACTB-1003 through regulating the expression of Fibroblast growth factor receptor 4 (FGFR4). [1], [2]
Ribosomal protein S6 kinase beta-1 (S6K1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Ribosomal protein S6 kinase beta-1 (S6K1) is a therapeutic target for ACTB-1003. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of ACTB-1003 through regulating the expression of Ribosomal protein S6 kinase beta-1 (S6K1). [3], [4]
References
Ref 1 N6-methyladenosine regulated FGFR4 attenuates ferroptotic cell death in recalcitrant HER2-positive breast cancer. Nat Commun. 2022 May 13;13(1):2672. doi: 10.1038/s41467-022-30217-7.
Ref 2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 3 m(6)A methyltransferase METTL3 promotes retinoblastoma progression via PI3K/AKT/mTOR pathway. J Cell Mol Med. 2020 Oct 8;24(21):12368-78. doi: 10.1111/jcmm.15736. Online ahead of print.
Ref 4 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83. doi: 10.1016/j.bmcl.2009.11.060. Epub 2009 Nov 20.