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. 2020 Nov 13;45(1):13–28. doi: 10.3892/or.2020.7851

Table II.

Physicochemical properties of approved ALK-TKIs.

Properties Crizotinib Ceritinib Brigatinib Alectinib Lorlatinib Entrectinib
Molecular formula (mg/mole) 450.34 558.14 584.10 482.62 406.41 560.64
Molecular weight C21H22Cl2FN5O C28H36ClN5O3S C29H39ClN7O2P C30H34N4O2 C21H19FN6O2 C31H34F2N6O2
Octanol/water 1.65 (pH 7.4) 5.23 5.17 NA 2.45 (pH 9) NA
Water solubility 0.00611 mg/ml 0.00222 mg/ml 0.022 mg/ml NA 32.38–0.17 (pH 2.55–8.02) NA
pKa 9.4 and 5.6 9.7 and 4.1 NA 7.05 (base) 4.9 NA

ALK-TKIs, anaplastic lymphoma kinase tyrosine kinase inhibitors; NA, not available; pKa, symbol for acid dissociation constant at logarithmic scale.