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Biological and Environmental Research Ontology
| Id | http://purl.obolibrary.org/obo/NCIT_C121817
http://purl.obolibrary.org/obo/NCIT_C121817
|
|---|---|
| Preferred Name | Samotolisib |
| Definitions |
An orally bioavailable, small molecule inhibitor of certain class I phosphoinositide 3-kinase (PI3K) isoforms and mammalian target of rapamycin kinase (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Samotolisib inhibits both certain PI3K isoforms and mTOR in an ATP-competitive manner which may inhibit both the PI3K/mTOR signaling pathway in and proliferation of tumor cells overexpressing PI3K and/or mTOR. The PI3K/mTOR pathway is upregulated in a variety of tumor cells and plays a key role in promoting cancer cell proliferation, and survival, motility and resistance to chemotherapy and radiotherapy. mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion; therefore, this agent may be more potent than an agent that inhibits either PI3K or mTOR alone. In addition, LY3023414 may inhibit DNA-dependent protein kinase (DNA-PK), thereby inhibiting the ability of tumor cells to repair damaged DNA. DNA-PK is activated upon DNA damage and plays a key role in repairing double-stranded DNA breaks.
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| Type | http://www.w3.org/2002/07/owl#Class |
All Properties
| definition | An orally bioavailable, small molecule inhibitor of certain class I phosphoinositide 3-kinase (PI3K) isoforms and mammalian target of rapamycin kinase (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Samotolisib inhibits both certain PI3K isoforms and mTOR in an ATP-competitive manner which may inhibit both the PI3K/mTOR signaling pathway in and proliferation of tumor cells overexpressing PI3K and/or mTOR. The PI3K/mTOR pathway is upregulated in a variety of tumor cells and plays a key role in promoting cancer cell proliferation, and survival, motility and resistance to chemotherapy and radiotherapy. mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion; therefore, this agent may be more potent than an agent that inhibits either PI3K or mTOR alone. In addition, LY3023414 may inhibit DNA-dependent protein kinase (DNA-PK), thereby inhibiting the ability of tumor cells to repair damaged DNA. DNA-PK is activated upon DNA damage and plays a key role in repairing double-stranded DNA breaks. |
|---|---|
| prefLabel | Samotolisib
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| label | Samotolisib
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| NCI_META_CUI | CL446628
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| PDQ_Closed_Trial_Search_ID | 738090
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| code | C121817
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| Has_Target | |
| prefixIRI | NCIT:C121817
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| in_subset |
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| Display_Name | Samotolisib
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| Preferred_Name | Samotolisib
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| FDA_UNII_Code | C88817F47Y
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| Contributing_Source |
CTRP
FDA
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| Maps_To | Samotolisib
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| CAS_Registry | 1386874-06-1
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| NCI_Drug_Dictionary_ID | 738090
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| type | |
| Is_Value_For_GDC_Property | |
| subClassOf | |
| PDQ_Open_Trial_Search_ID | 738090
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| Semantic_Type | Pharmacologic Substance
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