tubulysin b

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID Source	ID
PubMed CID	12134545
CHEMBL ID	1212995
CHEBI ID	80035
SCHEMBL ID	10063296
MeSH ID	M0543043

Synonyms (16)

Synonym
chebi:80035 ,
CHEMBL1212995
tubulysin b ,
SCHEMBL10063296
AKOS026674012
205304-87-6
benzenepentanoic acid, .gamma.-(((2-((1r,3r)-1-(acetyloxy)-4-methyl-3-(((2s,3s)-3-methyl-2-((((2r)-1-methyl-2-piperidinyl)carbonyl)amino)-1-oxopentyl)((1-oxobutoxy)methyl)amino)pentyl)-4-thiazolyl)carbonyl)amino)-4-hydroxy-.alpha.-methyl-, (.alpha.s,.gamm
Q27149182
EX-A5466
benzenepentanoic acid, gamma-(((2-((1r,3r)-1-(acetyloxy)-4-methyl-3-(((2s,3s)-3-methyl-2-((((2r)-1-methyl-2-piperidinyl)carbonyl)amino)-1-oxopentyl)((1-oxobutoxy)methyl)amino)pentyl)-4-thiazolyl)carbonyl)amino)-4-hydroxy-alpha-methyl-, (alphas,.gam
44d2d2m50t ,
unii-44d2d2m50t
HY-N1243
CS-0016644
(2s,4r)-4-[[2-[(1r,3r)-1-acetyloxy-3-[butanoyloxymethyl-[(2s,3s)-3-methyl-2-[[(2r)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]-4-methylpentyl]-1,3-thiazole-4-carbonyl]amino]-5-(4-hydroxyphenyl)-2-methylpentanoic acid
DTXSID901319116

Research Excerpts

Dosage Studied

Excerpt	Relevance	Reference
" This method was successfully used to determine concentration of EC1456 and its metabolites tubulysin B hydrazide and tubulysin B in tumor homogenates in preliminary experiments with KB tumor bearing mice dosed intravenously with EC1456."	( Development and validation of a UPLC-MS/MS method for the novel folate-targeted small molecule drug conjugate EC1456 and its metabolites in tumor homogenates from mice. Klein, PJ; Leamon, CP; Nelson, M; Pugh, M; Rao, SI; Reddy, JA, 2016)	0.65

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

Class	Description
butyrate ester	Any carboxylic ester where the carboxylic acid component is butyric acid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (11)

Assay ID	Title	Year	Journal	Article
AID495060	Binding affinity to wild type Angiococcus disciformis PKS/NRPS R27A/R29A mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID495057	Binding affinity to wild type Angiococcus disciformis PKS/NRPS R29A mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID1154048	Effect on spindle formation in mouse L929 cells at 3 ng/ml by impedance profiling	2014	Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13	SAR studies on hydropentalene derivatives--Important core units of biologically active tetramic acid macrolactams and ptychanolides.
AID495059	Binding affinity to wild type Angiococcus disciformis PKS/NRPS R20A/R29A mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID495054	Binding affinity to wild type Angiococcus disciformis PKS/NRPS expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID495056	Binding affinity to wild type Angiococcus disciformis PKS/NRPS R27A mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID495058	Binding affinity to wild type Angiococcus disciformis PKS/NRPS R20A/R27A mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID495055	Binding affinity to wild type Angiococcus disciformis PKS/NRPS R20A mutant expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID495053	Binding affinity to wild type Angiococcus disciformis PKS/NRPS expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry	2008	Nature chemical biology, Jan, Volume: 4, Issue:1	Multienzyme docking in hybrid megasynthetases.
AID1154045	Effect on microtubule polymerization in mouse L929 cells at 3 ng/ml by impedance profiling	2014	Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13	SAR studies on hydropentalene derivatives--Important core units of biologically active tetramic acid macrolactams and ptychanolides.
AID626425	Growth inhibition of human KB cells by [3H]thymidine incorporation assay	2011	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22	Acid mediated formation of an N-acyliminium ion from tubulysins: a new methodology for the synthesis of natural tubulysins and their analogs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	2 (15.38)	29.6817
2010's	11 (84.62)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.26

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.

Metric	This Compound (vs All)
Research Demand Index	20.26 (24.57)
Research Supply Index	2.64 (2.92)
Research Growth Index	5.27 (4.65)
Search Engine Demand Index	15.26 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (20.26)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	13 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
acetic acid Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed). acetic acid : A simple monocarboxylic acid containing two carbons.	2.06	1	monocarboxylic acid	antimicrobial food preservative; Daphnia magna metabolite; food acidity regulator; protic solvent
thymine [no description available]	2.17	1	pyrimidine nucleobase; pyrimidone	Escherichia coli metabolite; human metabolite; mouse metabolite
hydrazine diamine : Any polyamine that contains two amino groups.	2.17	1	azane; hydrazines	EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.17	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
substance p [no description available]	2.15	1	peptide	neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent
topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.	2.17	1	pyranoindolizinoquinoline	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor
docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.	2.17	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
carboplatin [no description available]	2.17	1
tubulysin a tubulysin A: has both antiangiogenic and antineoplastic activities; structure in first source	2.06	1	carboxylic acid; diester
folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.	2.84	3	folic acids; N-acyl-amino acid	human metabolite; mouse metabolite; nutrient

Condition	Relationship Strength	Studies
Neuroendocrine Tumors Tumors whose cells possess secretory granules and originate from the neuroectoderm, i.e., the cells of the ectoblast or epiblast that program the neuroendocrine system. Common properties across most neuroendocrine tumors include ectopic hormone production (often via APUD CELLS), the presence of tumor-associated antigens, and isozyme composition.	2.15	1
Benign Neoplasms [description not available]	2.85	3
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	2.85	3
Breast Cancer [description not available]	2.17	1
Cancer of Ovary [description not available]	2.17	1
Cancer of Prostate [description not available]	2.59	2
Cancer of Endometrium [description not available]	2.17	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.17	1
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	2.17	1
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	2.59	2
Endometrial Neoplasms Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells.	2.17	1

chemdatabank.com