| Description: |
Pacritinib (SB1518) is a potent and selective JAK2 (IC50 = 23 and 19 nM For JAK2(WT) and JAK2(V617F), respectively) and FLT3 (IC(50) = 22 nM) inhibitor with selectivity against JAK1 and JAK3 (IC(50) = 1280 and 520 nM, respectively).
IC50 Value: 23 nM (JAK2 wt); 22 nM (FLT3)
Target: JAK2; FLT3
in vitro: SB1518 shows potent effects on cellular JAK/STAT pathways, inhibiting tyrosine phosphorylation on JAK2 (Y221) and downstream STATs. As a consequence SB1518 has potent anti-proliferative effects on myeloid and lymphoid cell lines driven by mutant or wild-type JAK2 or FLT3, resulting from cell cycle arrest and induction of apoptosis .
in vivo: SB1518 has favorable pharmacokinetic properties after oral dosing in mice, is well tolerated and significantly reduces splenomegaly and hepatomegaly in a JAK2(V617F)-driven disease model. SB1518 dose-dependently inhibits intra-tumor JAK2/STAT5 signaling, leading to tumor growth inhibition in a subcutaneous model generated with SET-2 cells derived from a JAK2(V617F) patient with megakaryoblastic leukemia . Oral administration of pacritinib in murine models of FLT3-ITD-driven AML led to significant inhibition of primary tumor growth and lung metastasis. Upregulation of JAK2 in FLT3-TKI-resistant AML cells was identified as a potential mechanism of resistance to selective FLT3 inhibition . Pracinostat and pacritinib in combination showed synergy on tumor growth, reduction of metastases and synergistically decreased JAK2 or FLT signaling, depending on the cellular context .For the detailed information of Pacritinib, the solubility of Pacritinib in water, the solubility of Pacritinib in DMSO, the solubility of Pacritinib in PBS buffer, the animal experiment (test) of Pacritinib, the cell expriment (test) of Pacritinib, the in vivo, in vitro and clinical trial test of Pacritinib, the EC50, IC50,and Affinity of Pacritinib, Please contact DC Chemicals. |
