DOLASTATIN 10

Modify Date: 2024-01-05 16:14:41

DOLASTATIN 10 Structure
DOLASTATIN 10 structure
Common Name DOLASTATIN 10
CAS Number 110417-88-4 Molecular Weight 785.091
Density 1.1±0.1 g/cm3 Boiling Point 903.6±65.0 °C at 760 mmHg
Molecular Formula C42H68N6O6S Melting Point N/A
MSDS N/A Flash Point 500.3±34.3 °C

 Use of DOLASTATIN 10


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

 Names

Name L-Valinamide, N,N-dimethyl-L-valyl-N-[2-methoxy-4-[2-[1- methoxy-2-methyl-3-oxo-3-[[2-phenyl-1-(2-thiazolyl)ethyl] amino]propyl]-1-pyrrolidinyl]-1-(1-methylpropyl)-4-oxobutyl]-N-methyl-, [2S-[1[1R*(R*),2S*],2R*[1S*,2S*,3(R*)]]]
Synonym More Synonyms

 DOLASTATIN 10 Biological Activity

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

 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)

 Synonyms

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