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An Entity of Type : owl:Class, within Data Space : linked.opendata.cz:8890 associated with source document(s)

AttributesValues
rdf:type
rdfs:label
  • Apomine
rdfs:subClassOf
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
  • Organophosphorus Compound
Preferred_Name
  • Apomine
UMLS_CUI
  • C0766100
CAS_Registry
  • 126411-13-0
FDA_UNII_Code
  • JQ95208805
Contributing_Source
  • FDA
ALT_DEFINITION
  • An anticancer drug that belongs to the family of drugs called bisphosphonates. It affects cancer cell receptors governing cell growth and cell death.NCI-GLOSS
PDQ_Open_Trial_Search_ID
  • 43447
PDQ_Closed_Trial_Search_ID
  • 43447
Chemical_Formula
  • C28H52O7P2
Legacy_Concept_Name
  • SR-45023A
FULL_SYN
  • Phosphonic acid, (2-(3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)ethylidene)bis-, tetrakis(1-methylethyl) EsterSNNCI
  • SR-45023A (Apomine)PTDCP20013
  • Tetraisopropyl-2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethylidene-1,1-diphosphonateSNNCI
  • ApominePTNCI
  • SR-45023APTNCI-GLOSSCDR0000046662
  • SR-45023ACNNCI
  • SKF 99085CNNCI
  • TETRAISOPROPYL 2-(3,5-DI-TERT-BUTYL-4-HYDROXYPHENYL)ETHYL-1,1-BIPHOSPHONATEPTFDAJQ95208805
DEFINITION
  • A 1,1-bisphosphonate ester with potential antineoplastic and hypocholesterolemic activities. SR-45023A binds to hydroxyapatite crystals in the bone matrix where it inhibits enzymatic activity of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, which is required for the formation of mevalonate, the precursor of cholesterol. Consequently, shortage of mevalonate impedes the synthesis of downstream isoprenoids that are essential for protein prenylation. This leads to the loss of activity of proteins involved in osteoclast function and cellular proliferation, such as Ras and Rho, leading to an inhibition of cellular proliferation, and induction of osteoclasts apoptosis. In addition, SR-45023A activates the farnesoid X activated receptor (FXR), a member of the nuclear hormone superfamily implicated in cholesterol metabolism and bile acid transport and may play a role in this agent's antineoplastic effect.NCI
code
  • C1873
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