Preferred Name

Pinometostat

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C103179

CAS_Registry

1380288-87-8

code

C103179

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C177537

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C63923

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978

Contributing_Source

CTRP

GDC

FDA

DEFINITION

A small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Upon intravenous administration, pinometostat specifically blocks the activity of the histone lysine-methyltransferase DOT1L, thereby inhibiting the methylation of nucleosomal histone H3 on lysine 79 (H3K79) that is bound to the mixed lineage leukemia (MLL) fusion protein which targets genes and blocks the expression of leukemogenic genes. This eventually leads to an induction of apoptosis in the leukemic cells bearing the MLL gene translocations. DOT1L, a non-SET domain-containing histone methyltransferase, specifically methylates H3K79 and plays a key role in normal cell differentiation and in the development of leukemia with MLL gene rearrangement on chromosome 11 and promotes the expression of leukemia-causing genes.

Display_Name

Pinometostat

FDA_UNII_Code

8V9YR09EF3

FULL_SYN

PINOMETOSTAT

DOT1L Inhibitor EPZ-5676

EPZ-5676

Pinometostat

Has_Target

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C73703

Is_Value_For_GDC_Property

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1909

label

Pinometostat

Maps_To

Pinometostat

NCI_Drug_Dictionary_ID

740411

PDQ_Closed_Trial_Search_ID

740411

PDQ_Open_Trial_Search_ID

740411

Preferred_Name

Pinometostat

prefixIRI

Thesaurus:C103179

prefLabel

Pinometostat

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C3641112

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C471

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