Dolastatin 10
DRACPC ID DRACPC0035
Active Ingredients Dolastatin 10
Description A tetrapeptide originally isolated from the marine mollusk Dolabella auricularia with potential antineoplastic activity. Binding to tubulin, Dolastatin 10 inhibits microtubule assembly, resulting in the formation of tubulin aggregates and inhibition of mitosis. This agent also induces tumor cell apoptosis through a mechanism involving bcl-2, an oncoprotein that is overexpressed in some cancers.
Synonyms B720389K560; Dolastatin-10; L-Valinamide, N,N-dimethyl-L-valyl-N-[2-methoxy-4-[2-[1- methoxy-2-methyl-3-oxo-3-[[2-phenyl-1-(2-thiazolyl)ethyl]amino]propyl]-1-pyrrolidinyl]-1-(1-methylpropyl)-4-oxobutyl]-N-methyl-, [2S-[1[1R*(R*),2S*],2R*[1S*,2S*,3(R*)]]]; Dolastatin 10
Type Small Molecule
Disease Sarcoma, Leukemia, Lymphoma, Liver Cancer, Kidney Cancer
Classification
Mitotic inhibitor Marine origin
Structure Information
Molecular Formula C42H68N6O6S
Molecular Weight 785.1
Active Sequence Not available
Sequence Length Not available
Modification Not available
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-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide
InChI InChI=1S/C42H68N6O6S/c1-13-28(6)37(47(10)42(52)35(26(2)3)45-40(51)36(27(4)5)46(8)9)33(53-11)25-34(49)48-22-17-20-32(48)38(54-12)29(7)39(50)44-31(41-43-21-23-55-41)24-30-18-15-14-16-19-30/h14-16,18-19,21,23,26-29,31-33,35-38H,13,17,20,22,24-25H2,1-12H3,(H,44,50)(H,45,51)/t28-,29+,31-,32-,33+,35-,36-,37-,38+/m0/s1
InChI_Key OFDNQWIFNXBECV-VFSYNPLYSA-N
SMILES CC(C)[C@H](NC([C@@H](N(C)C)C(C)C)=O)C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N1[C@H]([C@H](OC)[C@@H](C)C(N[C@H](C2=NC=CS2)CC3=CC=CC=C3)=O)CCC1)=O)C)=O
External Codes
PubChem CID 9810929
DrugBank Accession Number DB12730
NCI Thesaurus Code C1300
UNII EI946JT51X GSRS
CAS 110417-88-4
Drug approval
Drug indication
Dolastatin 10 has been used in trials studying the treatment of Sarcoma, Leukemia, Lymphoma, Liver Cancer, and Kidney Cancer, among others.
The drug is not approved.
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT00003677 | Phase II Study of Dolastatin 10 (NSC# 376128) Administered Intravenously Every 21 Days to Patients With Metastatic Pancreatic Adenocarcinoma | Pancreatic Cancer | Phase 2 | Treatment |
| NCT00003778 | Phase II Trial of Dolastatin-10 in Patients With Previously Untreated Recurrent/Metastatic Sarcoma | Ovarian Cancer; Sarcoma | Phase 2 | Treatment |
| NCT00003557 | A Phase II Trial of Dolastatin-10 (NSC 376128) Administered as an IV Bolus Every 3 Weeks in Patients With Hepatobiliary Cancer | Extrahepatic Bile Duct Cancer; Gallbladder Cancer; Liver Cancer | Phase 2 | Treatment |
| NCT00003914 | Phase II Study of Dolastatin-10 in Patients With Advanced Renal Cell Carcinoma | Kidney Cancer | Phase 2 | Treatment |
| NCT00003693 | Phase I Study of Dolastatin-10 in Acute Leukemias, Myelodysplastic Syndromes and Chronic Myeloid Leukemia in Blast Phase | Leukemia; Myelodysplastic Syndromes | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
