Tubulysin D
Tubulysin D is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin D can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin D displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin D inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis.
For research use only. We do not sell to patients.
- CAS No.: 309935-57-7
- Formula: C43H65N5O9S
- Molecular Weight:828.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 1.7 μM (Tubulin)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.013 nM
Compound: 1b
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 21106374] |
| HCT-116 | IC50 |
0.0031 nM
Compound: 1b
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 21106374] |
| HL-60 | IC50 |
0.0047 nM
Compound: 1b
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 21106374] |
| KB-V1 | IC50 |
0.31 nM
Compound: 2
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Anticancer activity against human KBV1 cells expressing P-gp
Anticancer activity against human KBV1 cells expressing P-gp
|
[PMID: 19102699] |
| KB-V1 | IC50 |
0.31 nM
Compound: 2, tubulysin D
|
Anticancer activity against multidrug-resistant human KBV1 cells
Anticancer activity against multidrug-resistant human KBV1 cells
|
[PMID: 18314944] |
| MCF7 | IC50 |
0.67 nM
Compound: 1b
|
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 21106374] |
Tubulysin D has IC50s of 4.7 pM, 3.1 pM, 670 pM and 13 pM for HL60, HCT116, MCF7, A549 cell lines antiproliferative activity, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 309935-57-7
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Molecular Weight 828.07
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Formula C43H65N5O9S
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SMILES
CC(O[C@@H](C1=NC(C(N[C@H](C[C@H](C)C(O)=O)CC2=CC=CC=C2)=O)=CS1)C[C@H](C(C)C)N(COC(CC(C)C)=O)C([C@@]([C@@H](C)CC)([H])NC([C@@H](CCCC3)N3C)=O)=O)=O
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Structure Classification
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Initial Source
Archangium geophyra、Angiococcus disciformis
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Shibue T, et al. Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline. Bioorg Med Chem Lett. 2011 Jan 1;21(1):431-4. [Content Brief]
[2]. Kubicek K, et al. The tubulin-bound structure of the antimitotic drug tubulysin. Angew Chem Int Ed Engl. 2010 Jun 28;49(28):4809-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)