Product Name :
MPI-0441138
Description:
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.
CAS:
827030-33-1
Molecular Weight:
299.{{Edoxaban} medchemexpress|{Edoxaban} Metabolic Enzyme/Protease|{Edoxaban} Biological Activity|{Edoxaban} Purity|{Edoxaban} supplier|{Edoxaban} Cancer} 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
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.
Additional information:
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.{{Lomustine} site|{Lomustine} Autophagy|{Lomustine} Biological Activity|{Lomustine} Purity|{Lomustine} supplier|{Lomustine} Autophagy} Furthermore, in nude mice, MPI-0441138 significantly inhibited the growth of human PC-3 prostate cancer xenografts .PMID:23399686 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.|
