A tyrosine kinase inhibitor that potently inhibits Bcr/Abl tyrosine kinase and is effective in the treatment of certain leukemias; ~20-fold more potent than imatinib in inhibiting Bcr/Abl (e.g.

Nilotinib – 5 mg

Brand:
Cayman
CAS:
641571-10-0
Storage:
-20
UN-No:
Non-Hazardous - /

Nilotinib is a second generation tyrosine kinase inhibitor that is reported to have been used in targeted therapy for cancer. Specifically, it potently inhibits Bcr/Abl tyrosine kinase and is effective in the treatment of chronic myeloid leukemia (MLL) or Philadelphia chromosome acute lymphoblastic leukemia (Ph+ ALL), even in patients who are resistant to the first generation drug, imatinib (Gleevec).{17486,17480,17482,17483} Nilotinib is ~20-fold more potent than imatinib in inhibiting both wild-type and mutant Bcr/Abl (e.g., IC50 = 15 versus 280 nM, respectively, for wild-type Bcr/Abl).{17481} Also, nilotinib regulates the gene expression for DNA helicase complex, cyclins, and cyclin-dependent kinases, inhibiting cell proliferation and decreasing progression through S phase, while imatinib does not.{17484}  

 

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SKU: 10010422 - 5 mg Category:

Description

A tyrosine kinase inhibitor that potently inhibits Bcr/Abl tyrosine kinase and is effective in the treatment of certain leukemias; ~20-fold more potent than imatinib in inhibiting Bcr/Abl (e.g., IC50 = 15 versus 280 nM, respectively)

Formal name: 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide

Synonyms:  AMN107

Molecular weight: 529.5

CAS: 641571-10-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling

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