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

General Information of Drug (ID: DMT10C2)

• Drug Name: AG1295 Drug Info
• Synonyms: 6,7-Dimethyl-2-phenylquinoxaline; 71897-07-9; ag1295; AG-1295; AG 1295; CHEMBL7724; TYRPHOSTIN AG 1295; BiomolKI_000019; Tyrphostin AG-1295; AC1Q4WCY; AC1L1CSX; ChemDiv2_000256; BiomolKI2_000029; AC1Q2O4Y; cid_2048; BMK1-C7; MLS001194710; SCHEMBL925674; IFLab1_005463; GTPL5914; AC1Q2E07; CHEBI:94668; BDBM33408; CTK2H8610; DTXSID10274351; MolPort-000-182-258; FQNCLVJEQCJWSU-UHFFFAOYSA-N; 2-Phenyl-6,7-dimethylquinoxaline; HMS1427I07; HMS3229M19; HMS2879L07; HMS1369L14; ZINC257983; HMS3428I13; API01003; 6,7-Dimethyl-2-phenyl-quinoxaline
• Cross-matching ID:
  PubChem CID: 2048
  ChEBI ID: CHEBI:94668
  CAS Number: CAS 71897-07-9
  TTD Drug ID: DMT10C2

Molecule-Related Drug Atlas

Drug(s) Targeting Platelet-derived growth factor receptor alpha (PDGFRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[4]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[5]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[6]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[7]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[8]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[9]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[13]

Drug(s) Targeting Platelet-derived growth factor receptor beta (PDGFRB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[14]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[4]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[15]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[8]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[16]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[17]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[18]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[19]

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	[20]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[21]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[22]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[23]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[24]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[25]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[20]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[26]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[27]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[14]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[28]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[21]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[29]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[30]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[23]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[31]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[32]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[33]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[34]

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	[1]
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Inhibitor	[2]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[3]

References

• [1] Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. Bioorg Med Chem. 2007 Mar 1;15(5):2187-97.
• [2] Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
• [3] Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase i... Bioorg Med Chem. 2009 Oct 15;17(20):7324-36.
• [4] Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [8] E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
• [9] The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
• [10] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [11] National Cancer Institute Drug Dictionary (drug id 452042).
• [12] Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
• [13] Clinical pipeline report, company report or official report of MedImmune (2011).
• [14] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [16] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [17] Company report (Neuronova)
• [18] Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
• [19] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [20] 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).
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [22] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [23] 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.
• [24] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [25] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [26] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [27] 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.
• [28] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [29] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [30] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [31] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [32] Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
• [33] Clinical pipeline report, company report or official report of Exelixis (2011).
• [34] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services