m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02020)
Name
Bemcentinib
Synonyms
R428; 1037624-75-1; BGB324; R-428; BGB-324; UNII-0ICW2LX8AS; (S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine; CHEMBL3809489; SYN1131; CS-1046; HY-15150; QC-11751; R 428; W-5845; Bemcentinib [USAN]; R428 (BGB324); Bemcentinib (USAN/INN); BemcentinibR428BGB324); SCHEMBL1639904; GTPL10478; BGB 324; DTXSID70673109; 1-(6,7-dihydro-5H-benzo[2,3]cyclohepta[2,4-d]pyridazin-3-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine; AMY16774; BCP21180; C30H34N8; EX-A1720; SYN-1131; BDBM50172079; NSC824183; s2841; WHO 10631; ZINC51951669; AKOS032947237; ACN-037541; DB12411; NSC-824183; SB16614; NCGC00386665-07; 1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N~3~-[(7S)-7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]-1H-1,2,4-triazole-3,5-diamine; 1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo(6,7)cyclohepta(1,2-C)pyridazin-3-yl)-N3-((7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl)-; AC-28444; AS-16270; KB-80319; D11438; Q27236818; BGB324; BGB-324; BGB 324; R 428; R-428; Bemcentinib; 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(S)-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulene-2-yl)-1H-1,2,4-triazole-3,5-diamine
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Status
Phase 2
Structure
Formula
C30H34N8
InChI
1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1
InChIKey
KXMZDGSRSGHMMK-VWLOTQADSA-N
PubChem CID
46215462
TTD Drug ID
D0U8XE
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
 Regulator Info 
Response Summary Tyrosine-protein kinase UFO (AXL) is a therapeutic target for Bemcentinib. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Bemcentinib 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
 Regulator Info 
Response Summary Tyrosine-protein kinase UFO (AXL) is a therapeutic target for Bemcentinib. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of Bemcentinib 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 Company report (Mirati Therapeutics: formerly MethylGene)
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.