PPI-2458

DRACPC ID  DRACPC0082

Active Ingredients   PPI-2458

Description  A synthetic derivative of fumagillin with antineoplastic and cytotoxic properties. PPI-2458 irreversibly inhibits the enzyme methionine aminopeptidase type 2 (MetAP2), thereby preventing abnormal cell growth and angiogenesis. PPI-2458 is reported to have a better toxicity profile compared to other agents of its class.

Synonyms  MetAP-2 Inhibitor PPI-2458; Methionine Aminopeptidase 2 Inhibitor PPI-2458; PPI-2458

Type  Small Molecule

Disease  Lymphoma, Solid tumors

Classification

  

MetAP-2 Inhibitor Amino acid and derivative

Structure Information


Molecular Formula  C22H36N2O6

Molecular Weight  424.5

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl ((R)-1-amino-3-methyl-1-oxobutan-2-yl)carbamate

InChI  InChI=1S/C22H36N2O6/c1-12(2)7-8-15-21(5,30-15)18-17(27-6)14(9-10-22(18)11-28-22)29-20(26)24-16(13(3)4)19(23)25/h7,13-18H,8-11H2,1-6H3,(H2,23,25)(H,24,26)/t14-,15-,16-,17-,18-,21+,22+/m1/s1

InChI_Key QBDVVYNLLXGUGN-XGTBZJOHSA-N

SMILES  O=C(N[C@@H](C(N)=O)C(C)C)O[C@H]1[C@H]([C@@]([C@@]2(C)O[C@@H]2C/C=C(C)/C)([H])[C@@]3(CC1)OC3)OC

External Codes


PubChem CID  6918653

DrugBank Accession Number  DB05864

NCI Thesaurus Code  C38129  

UNII  NA0Y2SRR29   GSRS

CAS  431077-35-9



Drug approval


Drug indication
    Investigated for use/treatment in lymphoma (non-hodgkin's) and solid tumors.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT00100347 A Phase 1 Dose Escalation Safety/Tolerance Study of PPI-2458 in Subjects With Non-Hodgkin's Lymphoma and Solid Tumors Non-Hodgkin's Lymphoma; Solid Tumors Phase 1 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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