dolastatin 10
- Product Name
- dolastatin 10
- CAS No.
- 110417-88-4
- Chemical Name
- dolastatin 10
- Synonyms
- DLS 10;CS-1367;Nsc376128;Dolastain10;B720389K560;dolastatin 10;Dolastatin 10 (NSC-376128);Dolastatin 10,DLS 10,NSC 376128;From dolabella auricularia (sea hare);Dolastatin 10,DLS 10,NSC 376128, >99%
- CBNumber
- CB61390632
- Molecular Formula
- C42H68N6O6S
- Formula Weight
- 785.09
- MOL File
- 110417-88-4.mol
dolastatin 10 Property
- 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)
Safety
- RIDADR
- 3172
- HazardClass
- 6.1(b)
- PackingGroup
- III
N-Bromosuccinimide Price
- Product number
- CS-1825
- Product name
- Dolastatin10
- Purity
- 98.52%
- Packaging
- 1mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- B1035
- Product name
- Dolastatin10
- Packaging
- 1mg
- Price
- $523
- Updated
- 2021/12/16
- Product number
- CS-1825
- Product name
- Dolastatin10
- Purity
- 98.52%
- Packaging
- 5mg
- Price
- $800
- Updated
- 2021/12/16
- Product number
- B1035
- Product name
- Dolastatin10
- Packaging
- 5mg
- Price
- $1425
- Updated
- 2021/12/16
- Product number
- CSN17468
- Product name
- Dolastatin10
- Packaging
- 1mg
- Price
- $279
- Updated
- 2021/12/16
dolastatin 10 Chemical Properties,Usage,Production
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 10 Preparation Products And Raw materials
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