An inhibitor of the receptor tyrosine kinases c-Abl

Imatinib (mesylate) – 100 mg

Brand:
Cayman
CAS:
220127-57-1
Storage:
-20
UN-No:
Non-Hazardous - /

Imatinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit.{47196} It inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit (IC50s = ~0.3 and ~0.1 μM, respectively).{47196,47197} Imatinib inhibits the proliferation of Bcr-Abl-dependent R10(–) cells (IC50s = ~35-40 nM) and HMC-1 cells expressing constitutively active c-Kit in a concentration-dependent manner.{47196, 20180} It prolongs survival in a mouse model of chronic myeloid leukemia when administered at a dose of 100 mg/kg twice per day.{20177} Imatinib (25 and 50 µM) also inhibits the replication of Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in Vero E6 cells.{57353} It reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, when used at a concentration of 10 µM via inhibition of IBV surface glycoprotein protein-induced syncytia formation and virus-cell fusion.{45828} Formulations containing imatinib have been used in the treatment of various cancers.  

 

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Description

An inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit; inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit (IC50s = ~0.3 and ~0.1 μM, respectively); inhibits the proliferation of Bcr-Abl-dependent R10(–) cells (IC50s = ~35-40 nM) and HMC-1 cells expressing constitutively active c-Kit in a concentration-dependent manner; prolongs survival in a mouse model of chronic myeloid leukemia at 100 mg/kg twice daily; inhibits replication of MERS-CoV and SARS-CoV in Vero E6 cells at 25 and 50 µM; reduces viral titers in IBV-infected Vero cells at 10 µM

Formal name: 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, monomethanesulfonate

Synonyms:  CGP57148B|STI-571

Molecular weight: 589.7

CAS: 220127-57-1

Purity: ≥98%

Formulation: A crystalline solid

Application||Product Type|Biochemicals|Antivirals|Entry/fusion Inhibitors||Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Immunology & Inflammation|Pulmonary Diseases|MERS||Research Area|Immunology & Inflammation|Pulmonary Diseases|SARS||Research Area|Infectious Disease|Viral Diseases|Coronaviruses

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