m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02207)
Name
PF-03814735
Synonyms
PF-03814735; 942490-07-5; PF 03814735; PF-3814735; PF03814735; Kinome_1769; MLS006010949; CHEMBL1983111; SB19308; NCGC00389594-01; KB-74441; SMR004703046; BCP0726000114; J3.628.238J; N-(2-(6-((4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1,2,3,4-tetrahydro-1,4-epiminonaphthalen-9-yl)-2-oxoethyl)acetamide; N-[2-(4-{[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino}-11-azatricyclo[6.2.1.0^{2,7}]undeca-2(7),3,5-trien-11-yl)-2-oxoethyl]acetamide
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Status
Discontinued in Phase 1
Structure
Formula
C23H25F3N6O2
InChI
1S/C23H25F3N6O2/c1-12(33)27-11-20(34)32-18-7-8-19(32)16-9-14(5-6-15(16)18)30-22-28-10-17(23(24,25)26)21(31-22)29-13-3-2-4-13/h5-6,9-10,13,18-19H,2-4,7-8,11H2,1H3,(H,27,33)(H2,28,29,30,31)/t18-,19+/m0/s1
InChIKey
RYYNGWLOYLRZLK-RBUKOAKNSA-N
PubChem CID
51346455
TTD Drug ID
D0H7AC
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.
Aurora kinase B (AURKB)
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Aurora kinase B (AURKB) is a therapeutic target for PF-03814735. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of PF-03814735 through regulating the expression of Aurora kinase B (AURKB). [1], [2]
References
Ref 1 ALKBH5 promotes the proliferation of renal cell carcinoma by regulating AURKB expression in an m(6)A-dependent manner. Ann Transl Med. 2020 May;8(10):646. doi: 10.21037/atm-20-3079.
Ref 2 SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17. doi: 10.1007/s00280-009-1076-8. Epub 2009 Aug 1.