Soblidotin

DRACPC ID  DRACPC0057

Active Ingredients   Soblidotin

Description  A tetrapeptide derivative of dolastatin 10. Soblidotin inhibits tubulin polymerization, resulting in cell cycle arrest and induction of apoptosis. It has a role as a microtubule-destabilising agent, an antineoplastic agent and an apoptosis inducer. It is functionally related to a 2-phenylethylamine and a L-valine.

Synonyms  Auristatin PE; TZT-1027; N(2)-(N,N-Dimethyl-valyl)-N-(2-methoxy-4-(2-(1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-(1-methylpropyl)-4-oxobutyl)-N-methyl-valinamide; Soblidotin

Type  Small Molecule

Disease  Sarcoma, Lung Cancer

Classification

  

Tubulin inhibitor Peptide and derivative

Structure Information


Molecular Formula  C39H67N5O6

Molecular Weight  702

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

IUPAC Name  (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-(2-phenylethylamino)propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide

InChI  InChI=1S/C39H67N5O6/c1-13-27(6)35(43(10)39(48)33(25(2)3)41-38(47)34(26(4)5)42(8)9)31(49-11)24-32(45)44-23-17-20-30(44)36(50-12)28(7)37(46)40-22-21-29-18-15-14-16-19-29/h14-16,18-19,25-28,30-31,33-36H,13,17,20-24H2,1-12H3,(H,40,46)(H,41,47)/t27-,28+,30-,31+,33-,34-,35-,36+/m0/s1

InChI_Key DZMVCVHATYROOS-ZBFGKEHZSA-N

SMILES  [H][C@@]1([C@@H]([C@H](C(NCCC2=CC=CC=C2)=O)C)OC)CCCN1C(C[C@H]([C@@H](N(C([C@H](C(C)C)NC([C@@H](N(C)C)C(C)C)=O)=O)C)[C@H](CC)C)OC)=O

External Codes


PubChem CID  6918315

DrugBank Accession Number  DB12677

NCI Thesaurus Code  C26672  

UNII  DQC51A0WQH   GSRS

CAS  149606-27-9



Drug approval


Drug indication
    Soblidotin has been used in trials studying the treatment of Sarcoma, Lung Cancer, and Unspecified Adult Solid Tumor.

    The drug is not approved.

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT00064220 A Phase II Study of Intravenous TZT-1027, Administered Weekly Times Two, Every Three Weeks, to Patients With Advanced or Metastatic Soft Tissue Sarcomas (STS) With Prior Exposure to Anthracycline-Based Chemotherapy Sarcoma Phase 2 Treatment
NCT00061854 A Phase II Study Of Intravenous TZT-1027, Administered Weekly Times Two, Every Three Weeks, To Patients With Progressive Locally Advanced Or Metastatic Non-Small Cell Lung Cancer (NSCLC) Following Treatment With Platinum-Based Chemotherapy Lung Cancer Phase 2 Treatment
NCT00072228 Phase I Study of Soblidotin and Gemcitabine in Patients With Locally Advanced or Metastatic Solid Tumors Unspecified Adult Solid Tumor, Protocol Specific Phase 1 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





DRACP is developed by Dr.Zheng's team.