Drug Information
| Drug General Information | Top | |||
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| Drug ID |
DI1L7M
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| Drug Name |
PF-06821497
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| Synonyms |
UNII-S4L4MM20B6; S4L4MM20B6; CHEMBL4080228; PF06821497; 1844849-10-0; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one; SCHEMBL17330426; GTPL10516; BDBM50246967; NSC800019; DB14799; HY-101571A; NSC-800019; compound 23a [PMID: 29211475]; CS-0092626; Q29209799; 1(2H)-Isoquinolinone, 5,8-dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one; CJD
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| Drug Type |
Small molecular drug
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| Indication | Diffuse large B-cell lymphoma [ICD-11: 2A81; ICD-10: C83.3; ICD-9: 200] | Phase 1 | [1] | |
| Follicular lymphoma [ICD-11: 2A80; ICD-9: 202] | Phase 1 | [1] | ||
| Prostate cancer [ICD-11: 2C82.0; ICD-9: 185] | Phase 1 | [1] | ||
| Small-cell lung cancer [ICD-11: 2C25.Y] | Phase 1 | [1] | ||
| Company |
Pfizer
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| Structure |
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Download2D MOL |
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| Formula |
C22H24Cl2N2O5
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| Canonical SMILES |
CC1=CC(=C(C(=O)N1)CN2CCC3=C(C=C(C(=C3C2=O)Cl)C(C4COC4)OC)Cl)OC
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| InChI |
1S/C22H24Cl2N2O5/c1-11-6-17(29-2)15(21(27)25-11)8-26-5-4-13-16(23)7-14(19(24)18(13)22(26)28)20(30-3)12-9-31-10-12/h6-7,12,20H,4-5,8-10H2,1-3H3,(H,25,27)/t20-/m1/s1
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| InChIKey |
RXCVUHMIWHRLDF-HXUWFJFHSA-N
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| CAS Number |
CAS 1844849-10-0
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| PubChem Compound ID | ||||
| Target and Pathway | Top | |||
|---|---|---|---|---|
| Target(s) | Enhancer of zeste homolog 2 (EZH2) | Target Info | Inhibitor | [2] |
| KEGG Pathway | MicroRNAs in cancer | |||
| NetPath Pathway | IL2 Signaling Pathway | |||
| Reactome | PRC2 methylates histones and DNA | |||
| Oxidative Stress Induced Senescence | ||||
| PKMTs methylate histone lysines | ||||
| WikiPathways | Interactome of polycomb repressive complex 2 (PRC2) | |||
| Endoderm Differentiation | ||||
| Integrated Pancreatic Cancer Pathway | ||||
| Histone Modifications | ||||
| Cell Differentiation - meta | ||||
| miRs in Muscle Cell Differentiation | ||||
| miR-targeted genes in muscle cell - TarBase | ||||
| miR-targeted genes in lymphocytes - TarBase | ||||
| miR-targeted genes in epithelium - TarBase | ||||
| References | Top | |||
|---|---|---|---|---|
| REF 1 | ClinicalTrials.gov (NCT03460977) PF-06821497 Treatment Of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma. U.S. National Institutes of Health. | |||
| REF 2 | Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497). J Med Chem. 2018 Feb 8;61(3):650-665. | |||
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