PACRITINIB
Pacritinib
CAS: 937272-79-2
Molecular Formula: C28H32N4O3
PACRITINIB - Names and Identifiers
PACRITINIB - Physico-chemical Properties
| Molecular Formula | C28H32N4O3 |
| Molar Mass | 472.58 |
| Density | 1.22±0.1 g/cm3(Predicted) |
| Boling Point | 694.3±65.0 °C(Predicted) |
| pKa | 9.56±0.20(Predicted) |
| Storage Condition | 2-8℃ |
| In vitro study | Pacritinib is an inhibitor of wild-type JAK2 and JAK2V617F (IC 50 is 19 nM), which is present at high frequency in MPD patients. Relative to JAK2,Pacritinib inhibited TYK2(IC 50 is 50 nM) by 2-fold and JAK3(IC 50 is 520 nM) by 23-fold, inhibition of JAK1(IC 50 is 50 nM) was 56-fold lower. Pacritinib effectively penetrates the downstream signaling pathway of cell regulation JAK2, whether receptor agonist activation or mutant activation. In JAK2WT- and jak2v617f-deficient cells, Pacritinib induces apoptosis, cell cycle arrest, and antiproliferative effects. Pacritinib inhibited Karpas 1106P and Ba/F3-JAK2V617F cell proliferation with IC 50 of 348 nM and 160 nM, respectively. Pacritinib inhibits the growth of internal colonies derived from erythrocytes and Myeloid Progenitors with an IC50 of 63 nM and 53 nM, respectively. SB1518 also inhibited FLT3 gene and mutation FLT3-D835Y(IC50 is 6 nM). In FLT3 gene internal tandem repeats (ITD), flt3-wild type cells and primary AML blasts, Pacritinib inhibits FLT3 phosphorylation and downstream STAT,MAPK and PI3K signaling. In FLT3-ITD cells containing MV4-11, Pacritinib dose-dependently reduced pFLT3,pSTAT5,PERK1/ 2 and pAKT with IC50 of 80 nM,40 nM,33 nM and 29 nM, respectively. Treatment of primary AML cells with Pacritinib for 3 hours dose-dependently reduced pFLT3,pSTAT3 and pSTAT5,IC 50 below 0.5 μm. In FLT3 mutant and FLT3-wt cells, Pacritinib induces apoptosis, cell cycle arrest and antiproliferative effects. Pacritinib inhibited the proliferation of FLT3-ITD cells containing MV4-11 and primary AML cells with an IC50 of 47 nM and 0.19-1.3 nM, respectively. Pacritinib is wild-type JAK2 and JAK2 SB1518 also inhibited FLT3 gene and mutation FLT3-D835Y(IC50 is 6 nM). In FLT3 gene internal tandem repeats (ITD), flt3-wild type cells and primary AML blasts, Pacritinib inhibits FLT3 phosphorylation and downstream STAT,MAPK and PI3K signaling. In FLT3-ITD cells containing MV4-11, Pacritinib dose-dependently reduced pFLT3,pSTAT5,PERK1/ 2 and pAKT with IC50 of 80 nM,40 nM,33 nM and 29 nM, respectively. Treatment of primary AML cells with Pacritinib for 3 hours dose-dependently reduced pFLT3,pSTAT3 and pSTAT5,IC 50 below 0.5 μm. In FLT3 mutant and FLT3-wt cells, Pacritinib induces apoptosis, cell cycle arrest and antiproliferative effects. Pacritinib inhibited the proliferation of FLT3-ITD cells containing MV4-11 and primary AML cells with an IC50 of 47 nM and 0.19-1.3 nM, respectively. |
| In vivo study | Pacritinib(150 mg/kg) Oral q.d. Significantly improved splenomegaly and liver symptoms, normalized 60% spleen weight and 92% liver weight, without significant weight loss or any hematologic toxicity in a JAK2 V617F SUP> Related xenograft model, these include thrombocytopenia and anemia. Pacritinib induced a dose-dependent inhibition of jak2v617f-dependent SET-2 xenograft growth (40% at 75 mg/kg and 150 at 61% mg/kg). Pacritinib was effective in the FLT3-ITD xenograft model at MV4-11. Treatment with Pacritinib once daily for 21 consecutive days induced dose-dependent tumor growth inhibition (38% at 25 mg/kg, 92% at 50 mg/kg, and 100 at 121% mg/kg). Complete tumor regression was observed in three out of ten and eight out of eight mice in the 50 and 100 mg/kg/day groups, respectively. Pacritinib(150 mg/kg) Oral q.d. To JAK2 V617F Pacritinib was effective in a FLT3-ITD xenograft model. Treatment with Pacritinib once daily for 21 consecutive days induced dose-dependent tumor growth inhibition (38% at 25 mg/kg, 92% at 50 mg/kg, and 100 at 121% mg/kg). Complete tumor regression was observed in three out of ten and eight out of eight mice in the 50 and 100 mg/kg/day groups, respectively. |
PACRITINIB - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.116 ml | 10.58 ml | 21.16 ml |
| 5 mM | 0.423 ml | 2.116 ml | 4.232 ml |
| 10 mM | 0.212 ml | 1.058 ml | 2.116 ml |
| 5 mM | 0.042 ml | 0.212 ml | 0.423 ml |
Last Update：2024-01-02 23:10:35
PACRITINIB - Reference Information
| biological activity | Pacritinib (SB1518) is an effective Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) selective inhibitor with IC50 of 23 and 22 nM respectively. Phase 3 Pacritinib (SB1518) is an effective selective Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) inhibitor. IC50 in cell-free test is 23 and 22 nM respectively. Phase 3. |
| in vitro study | Pacritinib is an inhibitor of wild-type JAK2 and JAK2V617F (IC 50 is 19 nM), and it is present at high frequency in MPD patients. Compared with JAK2, the inhibitory effect of Pacritinib on TYK2(IC 50 is 50 nM) is 2 times lower, the inhibitory effect on JAK3(IC 50 is 520 nM) is 23 times lower, and the inhibitory effect on JAK1(IC 50 is 50 nM) is 56 times lower. Pacritinib effectively osmotic cells regulate the downstream signaling pathway of JAK2, whether it is receptor agonist activation or mutant activation. In JAK2WT- and JAK2V617F-deficient cells, apoptosis, cell cycle arrest and antiproliferative effects are Pacritinib induced. Pacritinib inhibited the proliferation of Karpas 1106P and Ba/F3-JAK2V617F cells, IC 50 was 348 nM and 160 nM respectively. The IC50 was Pacritinib 63 nM and 53 nM from inhibiting the growth of endogenous colonies derived from erythrocytes and myeloid progenitor cells, respectively. SB1518 also inhibits FLT3 gene and mutant FLT3-D835Y(IC50 is 6 nM). Pacritinib inhibits FLT3 phosphorylation and downstream STAT,MAPK, and PI3K signaling in FLT3 gene internal tandem repeats (ITD),FLT3-wild-type cells, and primary AML primordial cells. Pacritinib dose-dependent reductions of pFLT3,pSTAT5,PERK1/ 2, and pAKT,IC50 were 80 nM,40 nM,33 nM, and 29 nM, respectively, in FLT3-ITD-containing MV4-11 cells. Pacritinib treatment of primary AML cells for 3 hours dose-dependent reductions in pFLT3,pSTAT3 and pSTAT5,IC 50 were lower than 0.5 μM. In FLT3 mutant and FLT3-wt cells, apoptosis, cell cycle arrest and antiproliferative effects are Pacritinib induced. Pacritinib inhibit the proliferation of FLT3-ITD-containing MV4-11 cells and primary AML cells with IC50 of 47 nM and 0.19-1.3 nM respectively. Pacritinib is wild type JAK2 and JAK2 SB1518 also inhibit FLT3 gene and mutation FLT3-D835Y(IC50 is 6 nM). Pacritinib inhibits FLT3 phosphorylation and downstream STAT,MAPK, and PI3K signaling in FLT3 gene internal tandem repeats (ITD),FLT3-wild-type cells, and primary AML primordial cells. Pacritinib dose-dependent reductions of pFLT3,pSTAT5,PERK1/ 2, and pAKT,IC50 were 80 nM,40 nM,33 nM, and 29 nM, respectively, in FLT3-ITD-containing MV4-11 cells. Pacritinib treatment of primary AML cells for 3 hours dose-dependent reductions in pFLT3,pSTAT3 and pSTAT5,IC 50 were lower than 0.5 μM. In FLT3 mutant and FLT3-wt cells, apoptosis, cell cycle arrest and antiproliferative effects are Pacritinib induced. Pacritinib inhibit the proliferation of FLT3-ITD-containing MV4-11 cells and primary AML cells with IC50 of 47 nM and 0.19-1.3 nM respectively. |
| in vivo study | Pacritinib(150 mg/kg) oral q.d. to JAK2 V617F SUP> related transplanted tumor model, it can significantly improve the symptoms of splenomegaly and liver, and normalize the 60% spleen weight and 92% liver weight, there was no significant weight loss or any hematological toxicity, including thrombocytopenia and anemia. Pacritinib induced dose-dependent inhibition of JAK2V617F-dependent growth of SET-2 xenografts (40% at 75 mg/kg and 61% at 150 mg/kg). Pacritinib is effective for FLT3-ITD MV4-11 xenograft models. Pacritinib treatment, once daily for 21 days, induced dose-dependent tumor growth inhibition (38% at 25 mg/kg, 92% at 50 mg/kg, and 121% at 100 mg/kg). Complete tumor regression was observed in 3/10 and 8/8 mice in the 50 and 100 mg/kg/day groups, respectively. Pacritinib(150 mg/kg) oral q.d. to JAK2 V617F Pacritinib is effective for FLT3-ITD MV4-11 xenograft model. Pacritinib treatment, once daily for 21 days, induced dose-dependent tumor growth inhibition (38% at 25 mg/kg, 92% at 50 mg/kg, and 121% at 100 mg/kg). Complete tumor regression was observed in 3/10 and 8/8 mice in the 50 and 100 mg/kg/day groups, respectively. |
| features | dual JAK2/FLT3 inhibitors are in phase 3 clinical stage for the treatment of myelofibrosis. |
| target | TargetValue FLT3 (d835y) (cell-free say) 6 nmjak2 (v617f) (cell-free say) 19 nmflt3 (cell-free say) 22 nmjak2 (cell-free say) 23 nmtyk2 (cell-free say) 50 nm |
| Target | Value |
| FLT3 (D835Y) (Cell-free assay) | 6 nM |
| JAK2 (V617F) (Cell-free assay) | 19 nM |
| FLT3 (Cell-free assay) | 22 nM |
| JAK2 (Cell-free assay) | 23 nM |
| TYK2 (Cell-free assay) | 50 nM |
Last Update：2024-04-09 21:54:55
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View History
PACRITINIB
COPOLYMER OF STYRENE AND DIVINYLBENZENE, BROMINATED
Naphazoline impurity A (N0200000)
丙烯酸2,2,3,3-四氟丙酯(含稳定剂MEHQ)
1H-咪唑并[4,5-d]哒嗪
Reactive Red F3B
3,3'-DIPHTHALIDE
COPOLYMER OF STYRENE AND DIVINYLBENZENE, BROMINATED
Naphazoline impurity A (N0200000)
丙烯酸2,2,3,3-四氟丙酯(含稳定剂MEHQ)
1H-咪唑并[4,5-d]哒嗪
Reactive Red F3B
3,3'-DIPHTHALIDE