Page last updated: 2024-11-12
dolastatin 15
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
dolastatin 15: from Dolabella auricularia; seven subunit depsipeptide [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9918978 |
| CHEMBL ID | 35769 |
| SCHEMBL ID | 187502 |
| MeSH ID | M0203662 |
Synonyms (24)
| Synonym |
|---|
| dolastatin 15 |
| 123884-00-4 |
| dolastatin 15, >=95% |
| dolostatin 15 |
| CHEMBL35769 |
| l-proline, 1-(1-(n-(n-(n,n-dimethyl-l-valyl)-l-valyl)-n-methyl-l-valyl)-l-prolyl)-, 1-((2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1h-pyrrol-1-yl)carbonyl)-2-methylpropyl ester, (s-(r*,r*))- |
| nsc 617668 |
| l-proline, 1-(1-(n-(n-(n,n-dimethyl-l-valyl)-l-valyl)-n-methyl-l-valyl)-l-propyl)-, 1-((2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1h-pyrrol-1-yl)carbonyl)-2-methylpropyl ester, (s-(r*,r*))- |
| j9zks885h5 , |
| unii-j9zks885h5 |
| SCHEMBL187502 |
| dolastatin-15 |
| mfcd00236968 |
| J-004993 |
| DTXSID30924629 |
| l-proline, n,n-dimethyl-l-valyl-l-valyl-n-methyl-l-valyl-l-prolyl-, (1s)-1-[[(2s)-2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1h-pyrrol-1-yl]carbonyl]-2-methylpropyl ester |
| [(2s)-1-[(2s)-2-benzyl-3-methoxy-5-oxo-2h-pyrrol-1-yl]-3-methyl-1-oxobutan-2-yl] (2s)-1-[(2s)-1-[(2s)-2-[[(2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxyl |
| l-proline, n,n-dimethyl-l-valyl-l-valyl-n-methyl-l-valyl-l-prolyl-, (1s)-1-(((2s)-2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1h-pyrrol-1-yl)carbonyl)-2-methylpropyl ester |
| dls-15 |
| (s)-1-((s)-2-benzyl-3-methoxy-5-oxo-2,5-dihydro-1h-pyrrol-1-yl)-3-methyl-1-oxobutan-2-yl n-dimethyl-l-valyl-l-valyl-n-methyl-l-valyl-l-prolyl-l-prolinate |
| HY-P1126 |
| CS-0027988 |
| bdbm50472220 |
| AKOS040741663 |
Research Excerpts
Overview
Dolastatin 15 (DL15) is a potent, tubulin-targeted, vinca-site binding, anticancer agent. It induces mitotic arrest and inhibit cell proliferation in a variety of cell types.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dolastatin 15 is a microtubule-destabilizing agent with analogues undergoing clinical evaluation." | ( Dolastatin 15 from a Marine Cyanobacterium Suppresses HIF-1α Mediated Cancer Cell Viability and Vascularization. Carney, TJ; Dang, LH; Gunasekera, SP; Luesch, H; Ma, JJ; Paul, VJ; Ratnayake, R, 2020) | 2.72 |
| "Dolastatin 15 (DL15) is a potent, tubulin-targeted, vinca-site binding, anticancer agent that induces mitotic arrest and inhibit cell proliferation in a variety of cell types. " | ( Mechanism of mitotic arrest induced by dolastatin 15 involves loss of tension across kinetochore pairs. Lopus, M, 2013) | 2.1 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " Plasma and urine were sampled to characterize the pharmacokinetic behavior of tasidotin." | ( Phase I and pharmacokinetic study of tasidotin hydrochloride (ILX651), a third-generation dolastatin-15 analogue, administered weekly for 3 weeks every 28 days in patients with advanced solid tumors. Bonate, PL; Chu, QS; DeBono, JS; Garrison, M; Hammond, LA; Jones, CB; McCreery, H; Mita, AC; Rowinsky, EK; Syed, S; Weiss, G; Weitman, S, 2006) | 0.33 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (18)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Tubulin beta-4A chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9680 | 10.0000 | AID1404293 |
| Tubulin beta chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 2.0529 | 10.0000 | AID1404293 |
| Tubulin alpha-3C chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9555 | 10.0000 | AID1404293 |
| Tubulin alpha-1B chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9555 | 10.0000 | AID1404293 |
| Tubulin alpha-4A chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9555 | 10.0000 | AID1404293 |
| Tubulin beta-4B chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9680 | 10.0000 | AID1404293 |
| Tubulin beta-3 chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.8945 | 10.0000 | AID1404293 |
| Tubulin beta-2A chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9680 | 10.0000 | AID1404293 |
| Tubulin beta-8 chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9680 | 10.0000 | AID1404293 |
| Tubulin beta-2B chain | Bos taurus (cattle) | IC50 (µMol) | 17.0000 | 0.2500 | 1.8838 | 8.7000 | AID214005 |
| Tubulin alpha-3E chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9555 | 10.0000 | AID1404293 |
| Tubulin alpha-1A chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9555 | 10.0000 | AID1404293 |
| Similar to alpha-tubulin isoform 1 | Bos taurus (cattle) | IC50 (µMol) | 17.0000 | 0.2500 | 1.8779 | 8.7000 | AID214005 |
| Similar to alpha-tubulin isoform 1 | Bos taurus (cattle) | IC50 (µMol) | 17.0000 | 0.2500 | 1.8656 | 8.7000 | AID214005 |
| Tubulin alpha-1C chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9555 | 10.0000 | AID1404293 |
| Tubulin beta-6 chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9680 | 10.0000 | AID1404293 |
| Tubulin beta-2B chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9680 | 10.0000 | AID1404293 |
| Tubulin beta-1 chain | Homo sapiens (human) | IC50 (µMol) | 23.0000 | 0.0005 | 1.9870 | 10.0000 | AID1404293 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (52)
Molecular Functions (21)
Ceullar Components (36)
Bioassays (10)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID736658 | Inhibition of goat brain tubulin polymerization incubated for 20 mins prior to GTP addition measured for 30 mins by 90 degree light scattering-based fluorescence spectrophotometric method | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death. |
| AID98899 | Inhibitory activity against growth of L1210 cell line | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9 | Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. |
| AID101573 | Inhibitory activity against growth of MCF-7 cell line | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9 | Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. |
| AID1404293 | Inhibition of tubulin polymerization (unknown origin) pretreated for 15 mins followed by GTP addition by spectrophotometric method | 2018 | Journal of natural products, 03-23, Volume: 81, Issue:3 | Marine Invertebrate Natural Products that Target Microtubules. |
| AID214005 | In vitro inhibition of tubulin polymerization measured as turbidity formed by centrifugation | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9 | Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. |
| AID423029 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1 | Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A. |
| AID383123 | Antiplasmodial activity against Plasmodium falciparum after 72 hrs | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Tetramic and tetronic acids: an update on new derivatives and biological aspects. |
| AID83753 | Inhibitory activity against growth of HT-29 cell line | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9 | Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15. |
| AID423035 | Cytotoxicity against human NCI-H460 cells | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1 | Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A. |
| AID152559 | Anticancer activity against lymphocytic leukemia P388 cells was determined | 1998 | Bioorganic & medicinal chemistry letters, Feb-17, Volume: 8, Issue:4 | Synthesis of Dolastatin 15 mimetic peptoids. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (37)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 16 (43.24) | 18.2507 |
| 2000's | 11 (29.73) | 29.6817 |
| 2010's | 9 (24.32) | 24.3611 |
| 2020's | 1 (2.70) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 18.30
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (18.30) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (10.53%) | 5.53% |
| Reviews | 5 (13.16%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 29 (76.32%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||