Dactolisib
Dactolisib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform, and serine/threonine-protein kinase mTOR. In addition, it is known to target serine/threonine-protein kinase ATR.
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Commercial
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Clinical
Clinical Trials
26 clinical trials
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Indications Phases 4
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Indications Phases 3
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Indications Phases 2
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Dactolisib |
| INN | dactolisib |
| Description | Dactolisib is an imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, a mTOR inhibitor and an antineoplastic agent. It is an imidazoquinoline, a nitrile, a member of quinolines, a ring assembly and a member of ureas. |
| Classification | Small molecule |
| Drug class | phosphatidylinositol 3-kinase (PI3K) inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | Cn1c(=O)n(-c2ccc(C(C)(C)C#N)cc2)c2c3cc(-c4cnc5ccccc5c4)ccc3ncc21 |
Identifiers
| PDB | — |
| CAS-ID | 915019-65-7 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1879463 |
| ChEBI ID | 71952 |
| PubChem CID | 11977753 |
| DrugBank | — |
| UNII ID | RUJ6Z9Y0DT (ChemIDplus, GSRS) |
Target
Agency Approved
MTOR
MTOR
Organism
Homo sapiens
Gene name
MTOR
Gene synonyms
FRAP, FRAP1, FRAP2, RAFT1, RAPT1
NCBI Gene ID
Protein name
serine/threonine-protein kinase mTOR
Protein synonyms
FK506 binding protein 12-rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP-rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, Mammalian target of rapamycin, Mechanistic target of rapamycin, mechanistic target of rapamycin (serine/threonine kinase), mTOR, Rapamycin and FKBP12 target 1, rapamycin associated protein FRAP2, Rapamycin target protein 1
Uniprot ID
Mouse ortholog
Mtor (56717)
serine/threonine-protein kinase mTOR (Q9JLN9)
Alternate
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Safety
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38 adverse events reported
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