EC50: 2 nM for caspase activation MPI-0441138 is an inducer of apoptosis and growth inhibition. Apoptosis or programmed cell death is a process that organisms use to eliminate excessive cells and to control cell numbers. Caspases, a family of cysteine proteases, plays a critical role for the initiation as well as execution of apoptosis. In vitro: MPI-0441138 was identified as a highly active inducer of apoptosis and as a potent inhibitor of cell proliferation in T47D cells. MPI-0441138 also inhibited tubulin polymerization and was effective in cells overexpressing ABC transporter Pgp-1. It was found that the methyl group on the nitrogen linker was critical for the apoptosis-inducing activity . In vivo: MPI-0441138 could inhibit tumor growth dose-dependently and produced >95% tumor growth inhibition with once weekly dosing at 10 mg/kg and was well tolerated. The maximum tolerated dose of MPI-0441138 was determined to be 25 mg/kg when dosed once weekly, resulting in a good therapeutic index of 2.5. In addition, MPI-0441138 at a dose of 2.5 mg/kg could produce 90% tumor growth inhibition in the MX-1 model when dosed once every day for 5 days for 2 weeks. Furthermore, in nude mice, MPI-0441138 significantly inhibited the growth of human PC-3 prostate cancer xenografts . Clinical trial: Up to now, MPI-0441138 is still in the preclinical development stage.

Product information

CAS Number: 827030-33-1

Molecular Weight: 299.75

Formula: C16H14ClN3O

Chemical Name: 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine

Smiles: COC1C=CC(=CC=1)N(C)C1=NC(Cl)=NC2C=CC=CC=21

InChiKey: CIPVUQSDDVFBPO-UHFFFAOYSA-N

InChi: InChI=1S/C16H14ClN3O/c1-20(11-7-9-12(21-2)10-8-11)15-13-5-3-4-6-14(13)18-16(17)19-15/h3-10H,1-2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.