Plocabulin

DRACPC ID  DRACPC0093

Active Ingredients   Plocabulin

Description  A marine-derived, synthetically produced compound with potential antineoplastic activity. Plocabulin covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death.

Synonyms  PM-060184; PM060184; Plocabulin

Type  Small Molecule

Disease  Solid Tumors, Advanced Colorectal Cancer

Classification

  

Microtubule inhibitor Peptide and derivative

Structure Information


Molecular Formula  C31H45N3O7

Molecular Weight  571.7

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  [(1Z,4S,6Z)-1-[[(2S)-2-[[(2Z,4Z,6E,8S)-8-[(2S)-5-methoxy-6-oxo-2,3-dihydropyran-2-yl]-6-methylnona-2,4,6-trienoyl]amino]-3,3-dimethylbutanoyl]amino]octa-1,6-dien-4-yl] carbamate

InChI  InChI=1S/C31H45N3O7/c1-8-9-14-23(40-30(32)38)15-12-19-33-28(36)27(31(4,5)6)34-26(35)16-11-10-13-21(2)20-22(3)24-17-18-25(39-7)29(37)41-24/h8-13,16,18-20,22-24,27H,14-15,17H2,1-7H3,(H2,32,38)(H,33,36)(H,34,35)/b9-8-,13-10-,16-11-,19-12-,21-20+/t22-,23-,24-,27+/m0/s1

InChI_Key IEKGSKLKBICCHQ-BDOJOPHNSA-N

SMILES  C/C=C\C[C@H](OC(N)=O)C/C=C\NC([C@H](C(C)(C)C)NC(/C=C\C=C/C(C)=C/[C@@H]([C@@H]1CC=C(C(O1)=O)OC)C)=O)=O

External Codes


PubChem CID  57788271

DrugBank Accession Number  Not available

NCI Thesaurus Code  C95888  

UNII  52Y8L60CR7   GSRS

CAS  960210-99-5



Drug approval


Drug indication
    Investigated for use/treatment in Solid Tumors, Advanced Colorectal Cancer.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT01299636 Phase I, Multicenter, Open-label, Dose-escalating, Clinical and Pharmacokinetic Study of PM060184 Administered Intravenously to Patients With Advanced Solid Tumors Solid Tumors Phase 1 Treatment
NCT03427268 A Phase II, Open-label, Multicentre Study of PM060184 in Patients With Advanced Colorectal Cancer After Standard Treatment. Advanced Colorectal Cancer Phase 2 Treatment
NCT02533674 Phase I Multicenter, Open-label, Clinical and Pharmacokinetic Study of PM060184 in Combination With Gemcitabine in Selected Patients With Advanced Solid Tumors Solid Tumors Phase 1 Other

    More clinical information is obtained from ClinicalTrials.gov.





DRACP is developed by Dr.Zheng's team.