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Original Research

Comprehensive kinase profile of pacritinib, a nonmyelosuppressive Janus kinase 2 inhibitor

, , , , &
Pages 11-19 | Published online: 16 Aug 2016

Figures & data

Figure 1 Simulated steady-state peak plasma concentration (Cmax) for plasma protein-bound and free pacritinib after administration of 400 mg daily dosage of pacritinib in humans.

Figure 1 Simulated steady-state peak plasma concentration (Cmax) for plasma protein-bound and free pacritinib after administration of 400 mg daily dosage of pacritinib in humans.

Table 1 Kinase inhibition profile for pacritinib at 100 nM concentrationTable Footnotea

Figure 2 Pacritinib activity kinome map.

Abbreviations: AGC, protein kinase A, G, C group; ARK, Beta-adrenergic receptor kinase; BRK, breast tumor kinase; CK1, casein kinase; CLK, CDC Like Kinase 1; CSF1R, colony-stimulating factor 1 receptor; FLT3, fms-like receptor tyrosine kinase 3; HIPK4, homeodomain-interacting protein kinase 4; IC50, half maximal inhibitory concentration; IRAK1, interleukin-1 receptor-associated kinase 1; JAK, Janus kinase; STE, homolog of sterile; TK, tyrosine kinase; TKL, tyrosine kinase-like group of kinases; TNK1, tyrosine kinase nonreceptor 1; TYK2, tyrosine kinase 2.
Figure 2 Pacritinib activity kinome map.

Table 2 Relative kinase profiles comparing pacritinib, momelotinib, ruxolitinib, and fedratinib