General Information of the Drug (ID: M6APDG01195)
Name
MGCD265
Synonyms
MGCD-265; 875337-44-3; MGCD265; MGCD-265 analog; MGCD 265; N-(3-fluoro-4-(2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide; UNII-93M6577H9D; CHEMBL254760; 93M6577H9D; n-(3-fluoro-4-(2-(1-methyl-1h-imidazol-4-yl)thieno(3,2-b)pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide; N-[(3-Fluoro-4-{[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)carbamothioyl]-2-phenylacetamide
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Status
Phase 2
Structure
Formula
C26H20FN5O2S2
InChI
1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35)
InChIKey
UFICVEHDQUKCEA-UHFFFAOYSA-N
PubChem CID
24901704
TTD Drug ID
D08FDX
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.
Tyrosine-protein kinase UFO (AXL)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Tyrosine-protein kinase UFO (AXL) is a therapeutic target for MGCD265. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of MGCD265 through regulating the expression of Tyrosine-protein kinase UFO (AXL). [1], [2]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Tyrosine-protein kinase UFO (AXL) is a therapeutic target for MGCD265. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of MGCD265 through regulating the expression of Tyrosine-protein kinase UFO (AXL). [2], [3]
References
Ref 1 METTL3 promotes ovarian carcinoma growth and invasion through the regulation of AXL translation and epithelial to mesenchymal transition. Gynecol Oncol. 2018 Nov;151(2):356-365. doi: 10.1016/j.ygyno.2018.09.015. Epub 2018 Sep 21.
Ref 2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 3 Leukemogenic Chromatin Alterations Promote AML Leukemia Stem Cells via a KDM4C-ALKBH5-AXL Signaling Axis. Cell Stem Cell. 2020 Jul 2;27(1):81-97.e8. doi: 10.1016/j.stem.2020.04.001. Epub 2020 May 12.