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Dolastatin 10 CAS: 110417-88-4

Category: Inhibitors
Product Name: Dolastatin 10
Cat No: I000427
CAS No: 110417-88-4
Synonyms: (2S)-2-[[(2R)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3S,4S)-3-methoxy-1-[(2S)-2-[(1R,2S)-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
Molecular Formula: C42H68N6O6S
Molecular Weight: 785.09
SMILES: None
InChI: None
InChIKey: None
Solubility: 10 mM in DMSO
Target: Microtubule/Tubulin
Storage: Store at -20°C
CAS 110417-88-4,Dolastatin 10
  • Description

Dolastatin 10 is a potent antimitotic peptide from a marine animal, strongly inhibits microtubule assembly. Dolastatin and Dolastatin's analogs are the cytotoxic components in Antibody-drug conjugates design (eg. cAC10-vcMMAE)
IC50 Value:
Target: Tubulin; ADCs
Dolastatin 10 consists of four amino acids (in order from the amino terminus: dolavaline, valine, dolaisoleucine, and dolaproine), three unique to D. auricularia, linked to an unusual primary amine (dolaphenine, probably derived from phenylalanine) at what would otherwise be its carboxyl terminus. Monomethylauristatin E (MMAE) is a synthetic dolastatin 10 derivative with pronounced activity and toxicity.
The anti-CD30 monoclonal antibody cAC10 conjugated to the cytotoxic agent monomethyl auristatin E, a synthetic analog of the tubulin polymerization inhibitor dolastatin.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications. Maderna A, Doroski M, Subramanyam C, Porte A, Leverett CA, Vetelino BC, Chen Z, Risley H, Parris K, Pandit J, Varghese AH, Shanker S, Song C, Sukuru SC, Farley KA, Wagenaar MM, Shapiro MJ, Musto S, Lam MH, Loganzo F, O'Donnell CJ.J Med Chem. 2014 Dec 26;57(24):10527-43. doi: 10.1021/jm501649k. Epub 2014 Dec 9. PMID: 25431858
2:A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death. Gajula PK, Asthana J, Panda D, Chakraborty TK.J Med Chem. 2013 Mar 28;56(6):2235-45. doi: 10.1021/jm3009629. Epub 2013 Mar 19. PMID: 23445405
3:Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications of dolastatin 10. Pettit GR, Hogan F, Toms S.J Nat Prod. 2011 May 27;74(5):962-8. doi: 10.1021/np1007334. Epub 2011 May 2. PMID: 21534541 Free PMC Article
4:Potentiation of the activity of cisplatin in a human colon tumour xenograft model by auristatin PYE, a structural modification of dolastatin 10. Prokopiou EM, Cooper PA, Pettit GR, Bibby MC, Shnyder SD.Mol Med Rep. 2010 Mar-Apr;3(2):309-13. doi: 10.3892/mmr_00000256. PMID: 21472238
5:Combinatorial strategies by marine cyanobacteria: symplostatin 4, an antimitotic natural dolastatin 10/15 hybrid that synergizes with the coproduced HDAC inhibitor largazole. Taori K, Liu Y, Paul VJ, Luesch H.Chembiochem. 2009 Jul 6;10(10):1634-9. doi: 10.1002/cbic.200900192. PMID: 19514039
6:Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative and inhibitor of tubulin polymerization, given weekly to advanced solid tumor patients for 3 weeks. Yamamoto N, Andoh M, Kawahara M, Fukuoka M, Niitani H.Cancer Sci. 2009 Feb;100(2):316-21. doi: 10.1111/j.1349-7006.2008.01023.x. PMID: 19068085 Free Article
7:Phase II Trial of Dolastatin-10, a Novel Anti-Tubulin Agent, in Metastatic Soft Tissue Sarcomas. von Mehren M, Balcerzak SP, Kraft AS, Edmonson JH, Okuno SH, Davey M, McLaughlin S, Beard MT, Rogatko A.Sarcoma. 2004;8(4):107-11. doi: 10.1080/13577140400009163. PMID: 18521404 Free PMC Article
8:Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative, for the treatment of patients with non-small cell lung cancer. Horti J, Juhasz E, Monostori Z, Maeda K, Eckhardt S, Bodrogi I.Cancer Chemother Pharmacol. 2008 Jun;62(1):173-80. doi: 10.1007/s00280-007-0665-7. Epub 2008 Jan 23. PMID: 18214483
9:Auristatin PYE, a novel synthetic derivative of dolastatin 10, is highly effective in human colon tumour models. Shnyder SD, Cooper PA, Millington NJ, Pettit GR, Bibby MC.Int J Oncol. 2007 Aug;31(2):353-60. PMID: 17611692
10:Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative and inhibitor of tubulin polymerization, which was administered to patients with advanced solid tumors on days 1 and 8 in 3-week courses. Tamura K, Nakagawa K, Kurata T, Satoh T, Nogami T, Takeda K, Mitsuoka S, Yoshimura N, Kudoh S, Negoro S, Fukuoka M.Cancer Chemother Pharmacol. 2007 Jul;60(2):285-93. Epub 2006 Nov 30. PMID: 17136542


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