Description
An ALK inhibitor (IC50 = 0.2 nM); selective for ALK over IGF-1R, InsR, STK22D, and FLT3 (IC50s = 8, 7, 23, and 60 nM, respectively) as well as a panel of 25 additional kinases (IC50s = >0.26 μM for all); inhibits the proliferation of Ba/F3 cells expressing the fusion protein NPM-ALK or ELM4-ALK (IC50s = 0.02 and 0.021 μM, respectively), as well as several crizotinib-resistant NPM-ALK and ELM4-ALK mutants; reduces tumor growth in an H2228 NSCLC rat xenograft model at 10 mg/kg per day and induces tumor regression at 25 mg/kg per day; induces tumor regression in a Karpas299 lymphoma rat xenograft model at 25 and 50 mg/kg per day
Formal name: 5-chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine
Synonyms: LDK 378
Molecular weight: 558.1
CAS: 1032900-25-6
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Cancer|Multidrug Resistance
