(R)-Crizotinib, CAS 877399-52-5

Formulation: A crystalline solid

Formal Name: 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine

Purity: ≥98%

Formula Markup: C21H22Cl2FN5O

Formula Weight: 450,3

Shelf life (days): 1460

CAS Number: 877399-52-5

Notes: (R)-Crizotinib is a dual inhibitor of c-Met and anaplastic lymphoma kinase (ALK; IC50s = 8 and 20 nM, respectively, in a cell-based assay).{22302} It is selective for c-Met and ALK over several other receptor- and non-receptor tyrosine kinases, including Ron, Tie2, Abl, LCK, and VEGFR2 (IC50s = 0.08, 0.448, 1.159, 2.741, and >10 µM, respectively). (R)-Crizotinib selectively inhibits the proliferation of cancer cell lines with MET amplifications over cancer cell lines with MET or EGFR mutations (IC50s = 5-10, 472-1,284, and 767-787 nM, respectively).{22301} It induces apoptosis in MET-amplified EBC-1 and NCI H1993 lung cancer cells when used at a concentration of 100 nM. (R)-Crizotinib (25 mg/kg) reduces tumor volume in an EBC-1 mouse xenograft model. Formulations containing crizotinib have been used in the treatment of metastatic, relapsed, or refractory ALK-positive cancers.

• Artikelnummer: CAY12087-100
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 12087-100
• Green Labware: Nein
• Verpackungseinheit: 100 mg
• Mengeneinheit: STK