220127-57-1 Imatinib methanesulfonate AKSci J10205
 
 
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  J10205    AKSci Reference Standard
Imatinib methanesulfonate
, >98% (HPLC)
 
Imatinib mesylate
Imatinib mesilate
4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate
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IDENTITY
CAS Number:220127-57-1
MDL Number:MFCD04307699
MF:C30H35N7O4S
MW:589.71
BRN:10229624
SPECIFICATIONS & PROPERTIES
Purity:>98% (HPLC)
Spectra:LCMS, HPLC
Physical Form:White to yellow powder
Melting Point:207-211°C
Long-Term Storage:Store long-term at -20°C

BIOLOGICAL INFO
Solubility:DMSO: 118mg/mL; H2O: 118mg/mL; EtOH: <1mg/mL
Application(s):Multi-target inhibitor of v-Abl, c-Kit and PDGFR
Form:Mesylate salt

REVIEW

 Gleevec (imatinib mesylate) is a protein-tyrosine kinase inhibitor that blocks the constitutive abnormal tyrosine kinase, Bcr-Abl tyrosine kinase, that is created by the Philadelphia chromosome abnormality found in CML. In colony formation assays using ex vivo peripheral blood and bone marrow samples, imatinib shows inhibition of bcr-abl positive colonies from CML patients. In vivo, it inhibits tumor growth of bcr-abl transfected murine myeloid cells as well as bcr-abl positive leukemia lines derived from CML patients in blast crisis. Imatinib is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-kit, and inhibits PDGF- and SCF-mediated cellular events. In vitro, imatinib inhibits proliferation and induces apoptosis in gastrointestinal stromal tumor (GIST) cells, which express an activating c-kit mutation.

REFERENCES
[1]Huang WC, et al. Glucosylceramide synthase inhibitor PDMP sensitizes chronic myeloid leukemia T315I mutant to Bcr-Abl inhibitor and cooperatively induces glycogen synthase kinase-3-regulated apoptosis. FASEB J, 2011, 25(10), 3661-3673.
[2] Todd JR, et al. The MAPK pathway functions as a redundant survival signal that reinforces the PI3K cascade in c-Kit mutant melanoma. Oncogene, 2012, ahead of print.
[3] Kruewel T, et al. Molecular characterization of c-Abl/c-Src kinase inhibitors targeted against murine tumour progenitor cells that express stem cell markers. PLoS One, 2010, 5(11), e14143.
[4] Landry WD, et al. Imatinib and Nilotinib inhibit Bcr-Abl-induced ROS through targeted degradation of the NADPH oxidase subunit p22phox. Leuk Res, 2012, ahead of print.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H302

Precautionary Statements
P264; P270; P301+P312; P330; P501


Current as of June 25, 2019

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


PubChem