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DOLASTATIN 10

Names

[ CAS No. ]:
110417-88-4

[ Name ]:
DOLASTATIN 10

[Synonym ]:
D-Valinamide, N,N-dimethyl-L-valyl-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(2-thiazolyl)ethyl]amino]propyl]-1-pyrrolidinyl]-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-
N,N-Dimethyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino}propyl]-1-pyrrolidinyl}-5-methyl-1-oxo-4-heptanyl]-N-methyl-D-valinamide
dolastatin 10
From dolabella auricularia (sea hare)
N,N-Dimethyl-L-valyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-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-methyl-D-valinamide

Biological Activity

[Description]:

Dolastatin 10 is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization.

[Related Catalog]:

Signaling Pathways >> Antibody-drug Conjugate >> ADC Cytotoxin
Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin
Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin
Natural Products >> Others
Peptides
Research Areas >> Cancer

[Target]

Tubulin[1]


[In Vitro]

Dolastatin 10 is a unique pentapeptide that isolated from the sea hare Dolabella auricularia. These in vitro data are quite comparable to those of Dolastatin 10 and Auristatin PE, each of which has GI50 values of 10−5-10−6 μg/mL (10−2-10−3 nM) against a similar minipanel of human cell lines[2]. The antibody-drug conjugate (ADC) comprises the anti-CD30 monoclonal antibody cAC10 conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), a synthetic analog of the tubulin polymerization inhibitor Dolastatin 10[3].

[References]

[1]. Pitot HC, et al. Phase I trial of dolastatin-10 (NSC 376128) in patients with advanced solid tumors. Clin Cancer Res. 1999 Mar;5(3):525-31.

[2]. Pettit GR, et al. Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications ofdolastatin 10. J Nat Prod. 2011 May 27;74(5):962-8.

[3]. Brentuximab vedotin. Drugs R D. 2011;11(1):85-95.


[Related Small Molecules]

alpha-Amanitin | Nocodazole | Monomethyl auristatin E | VcMMAE | Mertansine | Campathecin | Calicheamicin | Eribulin mesylate | Daun02 | Epothilone D | Vinorelbine (ditartrate) | epothilone B | McMMAF | MMAF (Hydrochloride) | Ixabepilone

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
903.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C42H68N6O6S

[ Molecular Weight ]:
785.091

[ Flash Point ]:
500.3±34.3 °C

[ Exact Mass ]:
784.492126

[ PSA ]:
161.65000

[ LogP ]:
6.44

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.537

[ Storage condition ]:
-20°C

Safety Information

[ RIDADR ]:
UN 3172

[ Packaging Group ]:
III

[ Hazard Class ]:
6.1(b)

Related Compounds