Identification | Back 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 Properties | Back 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 Information | Back 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 |
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