Basic information Safety Supplier Related

dolastatin 10

Basic information Safety Supplier Related

dolastatin 10 Basic information

Product Name:
dolastatin 10
Synonyms:
  • (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
  • Dolastain10
  • Dolastatin 10 (NSC-376128)
  • 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-
  • dolastatin 10
  • B720389K560
  • From dolabella auricularia (sea hare)
  • 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*)]]]-
CAS:
110417-88-4
MF:
C42H68N6O6S
MW:
785.09
Product Categories:
  • ADCs
Mol File:
110417-88-4.mol
More
Less

dolastatin 10 Chemical Properties

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)
More
Less

Safety Information

RIDADR 
3172
HazardClass 
6.1(b)
PackingGroup 
III
More
Less

dolastatin 10 Usage And Synthesis

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.

dolastatin 10Supplier

Alabiochem Tech.Co., Ltd.
Tel
0512-58900862 400-0707518
Email
sales@alabiochem.com
Artis Chemistry (Shanghai) Co. Ltd.
Tel
86-21-60936353
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn