Drug Information
Drug (ID: DG01468) and It's Reported Resistant Information
Name |
PD98059
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Synonyms |
167869-21-8; PD 98059; PD98059; 2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one; PD 98,059; PD-98059; 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one; 2-(2-amino-3-methoxyphenyl)chromen-4-one; 2'-AMINO-3'-METHOXYFLAVONE; PD-098059; 4H-1-Benzopyran-4-one, 2-(2-Amino-3-methoxyphenyl)-; UNII-SJE1IO5E3I; SJE1IO5E3I; CHEMBL35482; C16H13NO3; CHEBI:77954; MFCD00671789; 2-(2-Amino-3-methoxy-phenyl)-chromen-4-one; SR-01000076097; PD 098059; 2-(2-Amino-3-methoxyphenyl)-chromen-4-one; NSC 679829; Tocris-1213; PD098059; Lopac-P-215; BiomolKI_000001; 2-(2-amino-3-methoxy-phenyl)chromen-4-one; BiomolKI2_000011; PD 98,059, solid; Lopac0_001028; BMK1-B1; BSPBio_000996; KBioGR_000336; KBioSS_000336; 2-(2'-amino-3'-methoxyphenyl)oxanaphthalen-4-one; MLS006010134; SCHEMBL157826; 4H-1-Benzopyran-4-one,2-(2-amino-3-methoxyphenyl)-; GTPL5241; QCR-14; 2''-amino-3''-methoxyflavone; BCBcMAP01_000049; KBio2_000336; KBio2_002904; KBio2_005472; KBio3_000671; KBio3_000672; AOB2598; DTXSID40168416; BCPP000123; Bio1_000475; Bio1_000964; Bio1_001453; Bio2_000338; Bio2_000818; HMS1362B17; HMS1792B17; HMS1990B17; HMS3229M08; HMS3263M17; HMS3267D03; HMS3403B17; HMS3412O09; HMS3649N14; HMS3654I16; HMS3676O09; BCP02423; EX-A2127; ZINC1420826; Tox21_501028; BDBM50108771; NSC679828; s1177; AKOS015995212; BCP9001060; BP34124; CCG-100605; CS-0169; LP01028; NSC 679828; NSC-679828; SB16629; SDCCGSBI-0051000.P003; IDI1_002093; SMP2_000052; NCGC00015790-01; NCGC00015790-02; NCGC00015790-03; NCGC00015790-04; NCGC00015790-05; NCGC00015790-06; NCGC00015790-07; NCGC00015790-08; NCGC00025045-01; NCGC00025045-02; NCGC00025045-03; NCGC00025045-04; NCGC00025045-05; NCGC00179347-01; NCGC00261713-01; AC-28412; AS-19374; HY-12028; NCI60_028554; SMR001456459; EU-0101028; FT-0716482; P-215; SW218254-2; X7398; EC-000.2425; A25454; P-4313; PD 98059 & Z-100; InSolution PD 98059 - CAS 167869-21-8; J-505513; SR-01000076097-1; SR-01000076097-3; SR-01000076097-6; 2-(2-amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran; BRD-K62810658-001-05-6; BRD-K62810658-001-06-4; Q27088281; 2-(2-Amino-3-methoxy-phenyl)-chromen-4-one(PD98059); PD 98059 - CAS 167869-21-8; 4H-1-Benzopyran-4-one, 2-(2-amino-3-methoxyphenyl)- & Z-100
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Indication |
In total 1 Indication(s)
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Structure | |||||
Drug Resistance Disease(s) |
Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug
(1 diseases)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
[2]
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Target | Phosphodiesterase 4D (PDE4D) | PDE4D_HUMAN | [3] | ||
Phosphodiesterase 5A (PDE5A) | PDE5A_HUMAN | [3] | |||
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Formula |
2
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IsoSMILES |
COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2
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InChI |
InChI=1S/C16H13NO3/c1-19-14-8-4-6-11(16(14)17)15-9-12(18)10-5-2-3-7-13(10)20-15/h2-9H,17H2,1H3
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InChIKey |
QFWCYNPOPKQOKV-UHFFFAOYSA-N
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PubChem CID | |||||
ChEBI ID | |||||
TTD Drug ID |
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
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.F53L (c.157T>C) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.F53L (c.157T>C) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.Q56P (c.167A>C) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.Q56P (c.167A>C) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.K57N (c.171G>C) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.K57N (c.171G>C) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.I111S (c.332T>G) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.I111S (c.332T>G) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.C121S (c.361T>A) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.C121S (c.361T>A) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.F129L (c.385T>C) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.F129L (c.385T>C) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: MAPK/ERK kinase 1 (MEK1) | [2] | |||
Molecule Alteration | Missense mutation | p.V211D (c.632T>A) |
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Resistant Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HEK293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 |
Experiment for Molecule Alteration |
SDS-PAGE assay | |||
Mechanism Description | The missense mutation p.V211D (c.632T>A) in gene MAP2K1 cause the resistance of PD98059 by unusual activation of pro-survival pathway |
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) | [3] | |||
Molecule Alteration | Missense mutation | p.K650E (c.1948A>G) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | NIH-3T3 cells | Embryo | Mus musculus (Mouse) | CVCL_0594 |
COS-1 cells | Kidney | Chlorocebus aethiops (Green monkey) | CVCL_0223 | |
Experiment for Molecule Alteration |
Immunoprecipitation and immunoblot analysis | |||
Mechanism Description | The missense mutation p.K650E (c.1948A>G) in gene FGFR3 cause the sensitivity of PD98059 by unusual activation of pro-survival pathway | |||
Key Molecule: Receptor-type tyrosine-protein kinase FLT3 (FLT3) | [4] | |||
Molecule Alteration | Missense mutation | p.R834Q (c.2501G>A) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | Bone marrow | N.A. | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Mechanism Description | The missense mutation p.R834Q (c.2501G>A) in gene FLT3 cause the sensitivity of PD98059 by aberration of the drug's therapeutic target |
Acute lymphocytic leukemia [ICD-11: 2B33]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Tyrosine-protein phosphatase non-receptor type 11 (PTPN11) | [1] | |||
Molecule Alteration | Missense mutation | p.E76K (c.226G>A) |
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Sensitive Disease | Acute lymphocytic leukemia [ICD-11: 2B33.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Experiment for Molecule Alteration |
Immunoblotting analysis | |||
Experiment for Drug Resistance |
Flow cytometry assay | |||
Mechanism Description | The missense mutation p.E76K (c.226G>A) in gene PTPN11 cause the sensitivity of PD98059 by unusual activation of pro-survival pathway |
References
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