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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
Molecular Weight:
785.09
MDL Number:
MFCD00870128
MOL File:
110417-88-4.mol
MSDS File:
SDS
Last updated:2023-05-21 10:59:17

dolastatin 10 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)
NCI Dictionary of Cancer Terms dolastatin 10
FDA UNII EI946JT51X
NCI Drug Dictionary dolastatin 10

SAFETY

Risk and Safety Statements

RIDADR  3172
HazardClass  6.1(b)
PackingGroup  III

dolastatin 10 price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ChemScene CS-1825 Dolastatin10 98.52% 110417-88-4 1mg $300 2021-12-16 Buy
ApexBio Technology B1035 Dolastatin10 110417-88-4 1mg $523 2021-12-16 Buy
ChemScene CS-1825 Dolastatin10 98.52% 110417-88-4 5mg $800 2021-12-16 Buy
ApexBio Technology B1035 Dolastatin10 110417-88-4 5mg $1425 2021-12-16 Buy
CSNpharm CSN17468 Dolastatin10 110417-88-4 1mg $279 2021-12-16 Buy
Product number Packaging Price Buy
CS-1825 1mg $300 Buy
B1035 1mg $523 Buy
CS-1825 5mg $800 Buy
B1035 5mg $1425 Buy
CSN17468 1mg $279 Buy

dolastatin 10 Chemical Properties,Uses,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.

13139-16-7
110417-88-4
Synthesis of dolastatin 10 from BOC-L-Isoleucine
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dolastatin 10 Spectrum

(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 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*)]]]- Nsc376128 DLS 10 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- CS-1367 Dolastatin 10,DLS 10,NSC 376128, >99% 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- 6-[bis[2-[(2-methylpropan-2-yl)oxycarbonylamino]ethyl] amino]-6-oxohexanoic acid (S)-2-((S)-2-(Dimethylamino)-3-methylbutanamido)-N-((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)-N,3-dimethylbutanamide ADC Cytotoxin,Dolastatin-10,Dolastatin 10,DLS10,inhibit,NSC376128,DLS-10,NSC-376128,Dolastatin10,Inhibitor,ADC Payload,Microtubule/Tubulin Dolastatin 10,DLS 10,NSC 376128 110417-88-4 C42H68N6O6S ADCs