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917369-31-4

917369-31-4 Structure

917369-31-4 Structure
IdentificationBack Directory
[Name]

N-(4-Methoxyphenyl)-N,2-dimethyl-4-quinazolinamine hydrochloride
[CAS]

917369-31-4
[Synonyms]

Azixa
EP-128495
MPC 6827 hydrochloride
Verubulin hydrochloride
N-(4-Methoxyphenyl)-N,2-dimethyl-4-quinazolinamine hydrochloride
N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine hydrochloride
[Molecular Formula]

C17H17N3O.HCl
[MDL Number]

MFCD22741413
[MOL File]

917369-31-4.mol
[Molecular Weight]

315.797
Chemical PropertiesBack Directory
[storage temp. ]

Desiccate at RT
[solubility ]

≥10.55 mg/mL in DMSO; ≥28.1 mg/mL in EtOH; ≥5 mg/mL in H2O
[form ]

Powder
[color ]

White to light yellow
Hazard InformationBack Directory
[Uses]

MPC 6827 Hydrochloride is a microtubule destabilizing agent which may be used in the treatment of patients with cancer.
[Biological Activity]

mpc-6827 (azixa) is a small-molecule microtubule-destabilizing agent that binds to the same (or nearby) sites on β-tubulin as colchicine.[1]tubulin is a heterodimer consisting of an αand βmonomer, it can be covalently labeled with [3h] colchicine by near uv irradiation. most of the label appears in β tubulin. colchicine binds to tubulin with a stoichiometry of one and inhibits microtubule assembly substoichiometrically. colchicine binding to tubulin exhibits pseudoirreversible kinetics; it displays a fast step followed by a slow step involving conformational changes of both ligand and tubulin. the tubulin, in turn, promotes fluorescence characteristic of the tropolone moiety of colchicine. [2]mpc-6827 is a small-molecule microtubule-destabilizing agent that causes mitotic arrest and cell death. mpc-6827 interfere with microtubule dynamics, leading to arrest of dividing cells in the g2-m phase of the cell cycle, which eventually results in apoptotic cell death.[1]
[in vivo]

mpc-6827 significantly inhibits the growth of various subcutaneously implanted tumor lines. mpc-6827 has also been shown to be a vascular-disrupting agent (vda) in a human ovarian carcinoma xenograft model. it also has shown synergism with carboplatin in a mouse xenograft model. furthermore, mpc-6827 has been shown to inhibit the growth of human glioblastoma tumor cell line (d-54) implanted intracranially in athymic nude mice. [1]
[storage]

Desiccate at RT
[References]

[1] tsimberidou am1, akerley w, schabel mc, etal. , phase i
Spectrum DetailBack Directory
[Spectrum Detail]

N-(4-Methoxyphenyl)-N,2-dimethyl-4-quinazolinamine hydrochloride(917369-31-4)1HNMR
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