Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMM5N8P)

• Drug Name: MRX-2843 Drug Info
• Synonyms: 1429882-07-4; UNC-2371A; UNII-2MT30EHI63; 2MT30EHI63; CHEMBL3326007; (1r,4r)-4-(2-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol; UNC2371A; SCHEMBL14854108; SCHEMBL17175579; BDBM350861; BCP30180; BDBM50055490; MFCD28502224; ZINC299829706; CS-8117; SB17283; AS-35252; HY-101549; US9795606, B20; A16958; UNC2371;UNC-2371;UNC 2371;MRX 2843 ;MRX2843; Cyclohexanol, 4-(2-((2-cyclopropylethyl)amino)-5-(4-((4-methyl-1-piperazinyl)methyl)phenyl)-7H-pyrrolo(2,3-d)pyrimidin-7-yl)-, trans-; trans-(1R,4R)-4-(2-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol; trans-4-(2-((2-Cyclopropylethyl)amino)-5-(4-((4-methyl-1-piperazinyl)methyl)phenyl)-7H-pyrrolo(2,3-d)pyrimidin-7-yl)cyclohexanol

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 89495685
  CAS Number: CAS 89495685
  TTD Drug ID: DMM5N8P

Molecule-Related Drug Atlas

Drug(s) Targeting Tyrosine-protein kinase Mer (MERTK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[3]
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[4]
ONO-7475	DMV6GX7	Acute leukaemia	2A60	Phase 1/2	[5]
RXDX-106	DM6NVTR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
PF-07265807	DMSMNRQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
INCB81776	DMFOXGB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
LDC1267	DMH7R6L	Discovery agent	N.A.	Investigative	[9]
G749	DMC7HIS	Discovery agent	N.A.	Investigative	[10]
UNC2025	DMCU59W	Glioblastoma of brain	2A00.00	Investigative	[11]
UNC569	DMJL6ZM	Acute lymphoblastic leukaemia	2A85	Investigative	[12]

Drug(s) Targeting Fms-like tyrosine kinase 3 (FLT-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[13]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[14]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[15]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[16]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[17]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[18]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[13]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[4]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[19]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[20]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[2]
Tyrosine-protein kinase Mer (MERTK)	TTO7LKR	MERTK_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT03510104) Pharmacokinetic and Safety Study of MRX-2843 in Adults With Relapsed/Refractory Advanced and/or Metastatic Solid Tumors. U.S. National Institutes of Health.
• [2] The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.
• [3] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Clinical pipeline report, company report or official report of Ono Pharmaceutical.
• [6] National Cancer Institute Drug Dictionary (drug name RXDX106).
• [7] National Cancer Institute Drug Dictionary (drug name PF-07265807).
• [8] A Potent and Selective Dual Inhibitor of AXL and MERTK Possesses Both Immunomodulatory and Tumor-Targeted Activity. Front Oncol. 2020 Dec 7;10:598477.
• [9] The E3 ligase Cbl-b and TAM receptors regulate cancer metastasis via natural killer cells. Nature. 2014 Mar 27;507(7493):508-12.
• [10] G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19.
• [11] MerTK as a therapeutic target in glioblastoma. Neuro Oncol. 2018 Jan 10;20(1):92-102.
• [12] UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77.
• [13] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1807).
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [15] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [16] A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
• [17] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [19] Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with ... Blood. 2008 Jun 15;111(12):5663-71.
• [20] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.