| Identification | Back Directory | [Name]
Tubulysin I | [CAS]
799822-10-9 | [Synonyms]
Tubulysin I
Benzenepentanoic acid, γ-[[[2-[(1R,3R)-1-(acetyloxy)-3-[[(acetyloxy)methyl][(2S,3S)-3-methyl-2-[[[(2R)-1-methyl-2-piperidinyl]carbonyl]amino]-1-oxopentyl]amino]-4-methylpentyl]-4-thiazolyl]carbonyl]amino]-4-hydroxy-α-methyl-, (αS,γR)- | [Molecular Formula]
C40H59N5O10S | [MDL Number]
MFCD32197436 | [MOL File]
799822-10-9.mol | [Molecular Weight]
801.99 |
| Chemical Properties | Back Directory | [Boiling point ]
967.4±65.0 °C(Predicted) | [density ]
1.222±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
4.52±0.23(Predicted) |
| Hazard Information | Back Directory | [Uses]
Tubulysin I is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin I can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin I displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin I inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis[1][2]. | [References]
[1] 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. DOI:10.1002/anie.200906828
[2] Vlahov IR, et al. Acid mediated formation of an N-acyliminium ion from tubulysins: a new methodology for the synthesis of natural tubulysins and their analogs. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6778-81. DOI:10.1016/j.bmcl.2011.09.041 |
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