dolastatin 10
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
dolastatin 10 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 activity
- -6829 (methanol)
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
- Tel
- 512-58900862 400-0707518
- sales@alabiochem.com
- Tel
- 86-21-60936353
- Tel
- 021-58170097
- info@topbiochem.com
- Tel
- 021-58950125
- info@chemexpress.com
- Tel
- 021-58955995
- sales@medchemexpress.cn
dolastatin 10(110417-88-4)Related Product Information
- (2S)-2-[[(2S)-2-dimethylamino-3-methyl-butanoyl]amino]-N-[(3R,4S,5S)-3 -methoxy-1-[(3R)-3-[(1R,2R)-1-methoxy-2-(phenethylcarbamoyl)propyl]pyr rolidin-1-yl]-5-methyl-1-oxo-heptan-4-yl]-N,3-dimethyl-butanamide
- Butanamide, 3-methyl-N-(4-oxo-4-(propylamino)butyl)-
- 4,9-dioxo-5,10-diazatetradecane
- N-Methylthiazole-2-methanamine
- dolastatin 10
- 2-(4-Aminopentyl(ethyl)amino)ethanol
- ETHYLENEDIAMINE TETRAKIS(PROPOXYLATE-BLOCK-ETHOXYLATE) TETROL