Drug (ID: DG01467) and It's Reported Resistant Information
Name
LY-294002
Synonyms
154447-36-6; LY294002; LY 294002; 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one; LY-294002; 2-morpholino-8-phenyl-4H-chromen-4-one; 2-morpholin-4-yl-8-phenyl-4H-chromen-4-one; UNII-31M2U1DVID; 2-morpholin-4-yl-8-phenylchromen-4-one; 2-(morpholin-4-yl)-8-phenylchromen-4-one; 15447-36-6; 2-(morpholin-4-yl)-8-phenyl-4H-chromen-4-one; NSC 697286; 31M2U1DVID; 2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE; CHEMBL98350; 4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl-; CHEBI:65329; SF 1101; LY2; Ly 294002 HCl; LY-294,002; 2-Morpholin-4-yl-8-phenyl-chromen-4-one; BMK1-D5; Lys 294002; 4azt; 2-morpholino-8-phenyl-chromen-4-one; Kinome_3543; Tocris-1130; 1yi3; BiomolKI_000029; Lopac-L-9908; 8-Phenyl-2-(morpholin-4-yl)-chromen-4-one; BiomolKI2_000037; CBiol_002046; Lopac0_000710; SCHEMBL94377; BSPBio_001223; KBioGR_000563; KBioSS_000563; MLS006010131; 2-Morpholino-8-phenylchromone; 2-(4-morpholino)-8-phenyl-4H-1-benzopyran-4-one; 4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl; GTPL6004; ZINC6014; DTXSID6042650; BCBcMAP01_000117; BDBM12915; KBio2_000563; KBio2_003131; KBio2_005699; KBio3_001005; KBio3_001006; EX-A073; SYN1108; BCPP000177; Bio1_000332; Bio1_000821; Bio1_001310; Bio2_000442; Bio2_000922; HMS1362M05; HMS1792M05; HMS1990M05; HMS3229G17; HMS3403M05; HMS3649E04; HMS3654M21; AMY40921; BCP00195; HSCI1_000206; NSC697286; NSC755769; s1105; AKOS017344742; BCP9000880; CCG-100633; CS-0150; DB02656; NSC-697286; NSC-755769; QC-7260; SB10965; SDCCGSBI-0050688.P003; SF-1101; IDI1_002197; NCGC00015622-01; NCGC00015622-02; NCGC00015622-03; NCGC00015622-04; NCGC00015622-05; NCGC00015622-06; NCGC00015622-07; NCGC00015622-23; NCGC00015622-27; NCGC00025020-01; NCGC00025020-02; NCGC00025020-03; NCGC00025020-04; NCGC00179253-01; AC-30295; AS-16252; HY-10108; NCI60_034712; SMR002530642; LY-924002; FT-0660382; M2410; SW217688-2; X7411; EC-000.2341; 2-Morpholino-8-phenyl-4-oxo-4H-1-benzopyran; K00235; J-510126; Q4042503; SR-01000076245-7; 4H-1-Benzopyran-4-one,2-(4-morpholinyl)-8-phenyl-; BRD-K27305650-001-05-9; InSolution LY 294002 - CAS 154447-36-6; LY-294,002 hydrochloride, solid, >=98% (HPLC); LY 294002 - CAS 154447-36-6; 4H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl- (9CI); H-1-Benzopyran-4-one, 2-(4-morpholinyl)-8-phenyl- (9CI); LY 294002; 2-(4-Morpholino)-8-phenyl-4H-1-benzopyran-4-one
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Indication
In total 1 Indication(s)
Diarrhea [ICD-11: DA90]
Phase 1
[1]
Structure
Target Opioid receptor delta (OPRD1) OPRD_HUMAN [2]
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Formula
2
IsoSMILES
C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
InChI
InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2
InChIKey
CZQHHVNHHHRRDU-UHFFFAOYSA-N
PubChem CID
3973
ChEBI ID
CHEBI:65329
TTD Drug ID
D0CS2F
DrugBank ID
DB02656
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
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Esophageal cancer [ICD-11: 2B70]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: PI3-kinase alpha (PIK3CA) [1]
Molecule Alteration Missense mutation
p.E545K (c.1633G>A)
Sensitive Disease Oesophagus adenocarcinoma [ICD-11: 2B70.0]
Experimental Note Identified from the Human Clinical Data
In Vitro Model TE cells Eye Oreochromis mossambicus (Mozambique tilapia) CVCL_YD05
KYSE cells N.A. . N.A.
Experiment for
Molecule Alteration
DNA sequencing assay
Experiment for
Drug Resistance
MTT assay
Mechanism Description The missense mutation p.E545K (c.1633G>A) in gene PIK3CA cause the sensitivity of LY-294002 by aberration of the drug's therapeutic target
Melanoma [ICD-11: 2C30]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Serine/threonine-protein kinase mTOR (mTOR) [2]
Molecule Alteration Missense mutation
p.H1968Y (c.5902C>T)
Sensitive Disease Melanoma [ICD-11: 2C30.0]
Experimental Note Identified from the Human Clinical Data
In Vitro Model HEK 292T cells Kidney Homo sapiens (Human) N.A.
Experiment for
Molecule Alteration
Western blotting analysis
Experiment for
Drug Resistance
CCK-8 assay
References
Ref 1 PIK3CA mutation status in Japanese esophageal squamous cell carcinomaJ Surg Res. 2008 Apr;145(2):320-6. doi: 10.1016/j.jss.2007.03.044. Epub 2008 Feb 11.
Ref 2 Analysis of mTOR Gene Aberrations in Melanoma Patients and Evaluation of Their Sensitivity to PI3K-AKT-mTOR Pathway InhibitorsClin Cancer Res. 2016 Feb 15;22(4):1018-27. doi: 10.1158/1078-0432.CCR-15-1110. Epub 2015 Oct 21.

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