Drug Information

Drug (ID: DG00830) and It's Reported Resistant Information

• Name: Trifluoperazine
• Synonyms: Trifluoperazine; Trifluperazine; 117-89-5; Trifluoroperazine; Trifluoperazin; Triflurin; Triperazine; Trifluoperazina; Flurazine; Trifluoromethylperazine; Stelazine; Trifluoperazinum; Trifluroperizine; Triphthasine; Eskazine; RP 7623; Fluoperazine; TFP; 10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)phenothiazine; Trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine; 10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)-10H-phenothiazine; NSC 17474; 10-(3-(4-methylpiperazin-1-yl)propyl)-2-(trifluoromethyl)-10H-phenothiazine; 10-[3-(4-Methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10H-phenothiazine; Calmazine; UNII-214IZI85K3; 10-(3-(4-Methyl-1-piperazinyl)propyl)-2-(trifluoromethyl)phenothiazine; 10H-Phenothiazine, 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-; 10-(gamma-(N'-Methylpiperazino)propyl)-2-trifluoromethylphenothiazine; 10-[3-(4-METHYL-PIPERAZIN-1-YL)-PROPYL]-2-TRIFLUOROMETHYL-10H-PHENOTHIAZINE; SKF 5019; CHEBI:45951; 214IZI85K3; 2-Trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine; 10H-Phenothiazine, 10-(3-(4-methyl-1-piperazinyl)propyl)-2-(trifluoromethyl)-; NSC-17474; NSC17474; Phenothiazine, 10-(3-(4-methyl-1-piperazinyl)propyl)-2-(trifluoromethyl)-; Trifluoperazina [Italian]; Apo-Trifluoperazine; Trifluoperazine [INN:BAN]; Trifluoperazinum [INN-Latin]; Trifluoperazina [INN-Spanish]; MLS001146870; MLS002702821; 10-(3-(4-methyl-1-piperazinyl)propyl)-2-(trifluoromethyl)-10H-phenothiazine; SMR001566649; CCRIS 6994; NSC-46061; C21H24F3N3S; HSDB 3195; Trifluoperazine (INN); 10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)phenothiazine dihydrochloride; CAS-440-17-5; EINECS 204-219-4; Apo-trifluoperazine (TN); NSC 46061; Stelazine (*Dihydrochloride*); 2-Trifluoromethyl-10-[3'-(1-methyl-4-piperazinyl)propyl]phenothiazine; Phenothiazine, 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-; NCI17474; Synklor (Salt/Mix); Stelazine (Salt/Mix); Triftazin (Salt/Mix); Spectrum_000668; Terfluzine (Salt/Mix); Triftazine (Salt/Mix); Jatroneural (Salt/Mix); Fluoperazine (Salt/Mix); Triphthazine (Salt/Mix); Prestwick0_000313; Prestwick1_000313; Prestwick2_000313; Prestwick3_000313; Spectrum2_000828; Spectrum3_001374; Spectrum4_000368; Spectrum5_001553; Lopac-T-8516; Biomol-NT_000060; CHEMBL422; cid_5566; 2-(((4-chlorophenyl)sulfonyl)amino)-benzoicaci; NCIStruc1_001127; NCIStruc2_001093; BIDD:PXR0132; Lopac0_001232; SCHEMBL24866; BSPBio_000306; BSPBio_001190; BSPBio_002928; GTPL214; KBioGR_000530; KBioGR_000835; KBioGR_002431; KBioSS_000530; KBioSS_001148; KBioSS_002437; MLS006011857; DivK1c_000843; SPBio_000755; SPBio_002525; BPBio1_000338; BPBio1_001345; DTXSID1046928; BDBM79181; cid_2913535; KBio1_000843; KBio2_000530; KBio2_001148; KBio2_002431; KBio2_003098; KBio2_003716; KBio2_004999; KBio2_005666; KBio2_006284; KBio2_007567; KBio3_000959; KBio3_000960; KBio3_002148; KBio3_002910; cMAP_000048; NINDS_000843; Bio1_000458; Bio1_000947; Bio1_001436; Bio2_000435; Bio2_000915; HMS1362L11; HMS1792L11; HMS1990L11; HMS2089J11; HMS3429O07; KUC109776N; BCP32898; EX-A3330; CCG-37306; NCGC00013226; PDSP1_001300; PDSP2_001284; s5856; STK182873; ZINC19418959; 10-(3-(4-methyl-1-piperazinyl)propyl)-2-(trifluoromethyl)-phenothiazine; AKOS001487920; DB00831; MCULE-3726407978; RP-7623; SDCCGSBI-0051199.P005; IDI1_000843; IDI1_002190; KSC-210-031; MRF-0000088; QTL1_000085; NCGC00013226-02; NCGC00013226-03; NCGC00013226-04; NCGC00013226-05; NCGC00013226-06; NCGC00013226-07; NCGC00013226-08; NCGC00013226-09; NCGC00013226-10; NCGC00013226-11; NCGC00013226-12; NCGC00013226-13; NCGC00013226-15; NCGC00013226-26; NCGC00024251-03; NCGC00024251-04; NCGC00024251-05; NCGC00024251-06; NCGC00024251-07; M989; NCI60_001427; NCI60_004087; SBI-0051199.P003; AB00053558; FT-0650159; C07168; D08636; AB00053558-27; AB00053558_28; AB00053558_29; L001075; Q1752915; SR-01000003020-6; BRD-K89732114-001-02-6; BRD-K89732114-001-03-4; BRD-K89732114-001-05-9; BRD-K89732114-300-05-5; BRD-K89732114-300-07-1; Triphthazine;Trifluperazine;NSC-17474;RP-7623;SKF-5019; 10-(.gamma.-(N'-Methylpiperazino)propyl)-2-trifluoromethylphenothiozine; 10-[3-(4-Methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10H-phenothiazine #; 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)phenothiazine;hydrochloride; 10-[3-(4-methylpiperazino)propyl]-2-(trifluoromethyl)phenothiazine;hydrochloride
• Indication:
  In total 1 Indication(s)
  Schizophrenia [ICD-11: 6A20]; Approved; [1]
• Target: Calmodulin (CALM); CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN; [1]
• Formula: C21H24F3N3S
• IsoSMILES: CN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)C(F)(F)F
• InChI: 1S/C21H24F3N3S/c1-25-11-13-26(14-12-25)9-4-10-27-17-5-2-3-6-19(17)28-20-8-7-16(15-18(20)27)21(22,23)24/h2-3,5-8,15H,4,9-14H2,1H3
• InChIKey: ZEWQUBUPAILYHI-UHFFFAOYSA-N
• PubChem CID: 5566
• ChEBI ID: CHEBI:45951
• TTD Drug ID: D0R4OM
• VARIDT ID: DR00664
• INTEDE ID: DR1641
• DrugBank ID: DB00831

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Multiple myeloma [ICD-11: 2A83]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Nuclear protein 1, transcriptional regulator (NUPR1) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Multiple myeloma [ICD-11: 2A83.0]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell autophagy; Activation; hsa04140
• Cell Pathway Regulation: Cell apoptosis; Activation; hsa04210
• In Vitro Model: HSC3 cells; Tongue; Homo sapiens (Human); CVCL_1288
• In Vitro Model: OVCAR3 cells; Ovary; Homo sapiens (Human); CVCL_0465
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: CCK8 assay
• Mechanism Description: There was statistical difference in the expression of the aforementioned proteins between the TFptreated group and TFptreated NC-LV group, but the autophagy level was upregulated and apoptosis was downregulated in the TFptreated NUPR1-LV group compared with the TFptreated NC-LV group. NUPR1 overexpression reversed the autophagic suppression and cellular apoptosis induction caused by TFP in U266 and RPMI 8226 cells. Thus, we concluded that TFP targeted NUPR1 in MM cells and subsequently induced apoptosis by inhibiting autophagy.

References

• Ref 1: Trifluoperazine induces cellular apoptosis by inhibiting autophagy and targeting NUPR1 in multiple myeloma .FEBS Open Bio. 2020 Oct;10(10):2097-2106. doi: 10.1002/2211-5463.12960. Epub 2020 Aug 31. 10.1002/2211-5463.12960