ChemicalBook CAS DataBase List 110417-88-4

110417-88-4

Name	dolastatin 10
CAS	110417-88-4
Molecular Formula	C42H68N6O6S
MDL Number	MFCD00870128
Molecular Weight	785.09
MOL File	110417-88-4.mol

Synonyms

DLS 10 CS-1367 Nsc376128 B720389K560 Dolastain10 dolastatin 10 Dolastatin 10 (NSC-376128) Dolastatin 10,DLS 10,NSC 376128, >99% From dolabella auricularia (sea hare) 6-[bis[2-[(2-methylpropan-2-yl)oxycarbonylamino]ethyl] amino]-6-oxohexanoic acid 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- L-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- 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*)]]]- (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-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,3-dimethylbutanamide

Chemical Properties

Melting point	107～112
Boiling point	903.6±65.0 °C(Predicted)
density	1.116±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C,unstable in solution, ready to use.
solubility	≥78.5 mg/mL in EtOH; insoluble in H2O; ≥67.2 mg/mL in DMSO
form	Powder
pka	13.81±0.46(Predicted)
color	White to off-white
Optical Rotation	-6829 (methanol)

Safety Data

RIDADR	3172
HazardClass	6.1(b)
PackingGroup	III

Hazard Information

Definition

ChEBI: Dolastatin 10 is a tetrapeptide that is isolated from the sea hare Dolabella auricularia. It is a potent anticancer agent which inhibits tubulin polymerization. It has a role as an animal metabolite, a marine metabolite, an antineoplastic agent, an apoptosis inducer and a microtubule-destabilising agent. It is a member of 1,3-thiazoles and a tetrapeptide. It is functionally related to a L-valine.

Biological Activity

dolastatin 10 is an antitumor agent [1].dolastatin 10 is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. dolastatin 10 is found to have activity to inhibit tubulin polymerization with ic50 value of 1.2μm. besides that, it potently inhibits vincristine binding to tubulin with a ki value of 1.4μm in a noncompetitive manner. dolastatin 10 also shows moderate effect on enhancing the binding of colchicines to tubulin. in addition, dolastatin 10 has the inhibitory activity in tubulin-dependent gtp binding [1].in the cellular assay, dolastatin 10 shows activity against some human leukaemia, lymphoma and solid tumour cell lines (such as ovcar-3 and nsclc) with ic50 values ranging from 0.1nm to 10nm. it is currently tested in the

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 GI < sub> 50 values of 10 ^?5 -10 ^?6 μg/mL (10 ^?2 -10 ^{? 3} nM) against a similar minipanel of human cell lines. 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.

target

Auristatin

References

[1] bai r l, pettit g r, hamel e. binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. journal of biological chemistry, 1990, 265(28): 17141-17149.
[2] schwartsmann g. marine organisms and other novel natural sources of new cancer drugs. annals of oncology, 2000, 11(suppl 3): 235-243.

Spectrum Detail

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