E7974

DRACPC ID  DRACPC0048

Active Ingredients   E7974

Description  An analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of existing microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype.

Synonyms  E-7974; E7974; Hemiasterlin Analog E7974

Type  Small Molecule

Disease  Cancer, Malignant Tumors

Classification

  

Peptide and derivative Marine origin

Structure Information


Molecular Formula  C24H43N3O4

Molecular Weight  437.6

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  (E,4S)-4-[[(2S)-3,3-dimethyl-2-[[(2R)-1-propan-2-ylpiperidine-2-carbonyl]amino]butanoyl]-methylamino]-2,5-dimethylhex-2-enoic acid

InChI  InChI=1S/C24H43N3O4/c1-15(2)19(14-17(5)23(30)31)26(9)22(29)20(24(6,7)8)25-21(28)18-12-10-11-13-27(18)16(3)4/h14-16,18-20H,10-13H2,1-9H3,(H,25,28)(H,30,31)/b17-14+/t18-,19-,20-/m1/s1

InChI_Key FWYMMXUDTATKLG-PGLMLKKXSA-N

SMILES  OC(/C(C)=C/[C@H](C(C)C)N(C)C([C@@H](NC([C@@H]1N(CCCC1)C(C)C)=O)C(C)(C)C)=O)=O

External Codes


PubChem CID  10127315

DrugBank Accession Number  Not available

NCI Thesaurus Code  C49083  

UNII  1BO0C11BSH   GSRS

CAS  610787-07-0



Drug approval


Drug indication
    Investigated for use/treatment in Cancer and Malignant Tumors.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT00165802 A Phase I Open Label Study of E7974 Administered on Day 1 of a 21-Day Cycle In Patients With Advanced Solid Tumors Cancer, Malignant Tumors Phase 1 Treatment
NCT00130169 A Phase 1 Open-Label Study of E7974 Administered on Days 1 and 15 of a 28-Day Cycle in Patients With Solid Malignancies Cancer, Malignant Tumors Phase 1 Treatment
NCT00121732 A Phase 1, Two-Arm, Open-Label Study of E7974 Administered on Days 1, 8, and 15 of a 28-Day Cycle and Days 1 and 8 of a 21-Day Cycle in Patients With Solid Malignancies Cancer, Malignant Tumors Phase 1 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





DRACP is developed by Dr.Zheng's team.