Pacritinib

Name Value
Weight 472.589 g/mol
Zinc ID ZINC43153645
Smiles C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2cccc(c2)COC/1
Molecular formula C28H32N4O3
Mode of inhibition JAK2; Tyrosine kinase inhibitor
CAS 937272-79-2

Clinical Trials

Study title Status Conditions Link
Determine Pacritinib Pharmacokinetics in Impaired Hepatic Patients and Healthy Subjects Completed Myelofibrosis NCT02765724
Investigate Absorption, Metabolism, Excretion, and Mass Balance of Pacritinib Completed Healthy NCT02803762
Pacritinib Combined With Decitabine or Cytarabine in Older Patients With AML Terminated Acute Myeloid Leukemia (AML) NCT02532010
To Evaluate the Effect of Clarithromycin on the Systemic Exposure of Pacritinib in Healthy Subjects Completed Drug Interaction Study NCT02807051
Drug-Interaction Study to Evaluate the Effect of Rifampin, a Potent CYP3A4 Inducer, on the Systemic Exposure of Pacritinib in Healthy Subjects Completed Healthy Subjects NCT02807116
Oral Pacritinib Versus Best Available Therapy to Treat Myelofibrosis With Thrombocytopenia Terminated Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis NCT02055781
Myelofibrosis Treated With Pacritinib Before aSCT. (HOVON134MF) Recruiting Myelofibrosis NCT03645824
A Phase 2/3 Study of Pacritinib in Patients With Primary Myelofibrosis, Post Polycythemia Vera Myelofibrosis, or Post-Essential Thrombocythemia Myelofibrosis Recruiting Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis NCT03165734
Oral Pacritinib Versus Best Available Therapy to Treat Myelofibrosis Terminated Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis NCT01773187
Pacritinib in Relapsed/Refractory Lymphoproliferative Disorders Recruiting Lymphoma, T-Cell, Cutaneous|Lymphoma, T-Cell, Peripheral|Chronic Lymphocytic Leukemia|Lymphoproliferative Disorders|Waldenstrom Macroglobulinemia|Lymphoplasmacytic Lymphoma|Mantle Cell Lymphoma NCT03601819
Multicenter Study of Pacritinib Combined With Ibrutinib in Relapsed/Refractory Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) Withdrawn Chronic Lymphocytic Leukemia|Lymphoma, Small Lymphocytic NCT02677948
Pacritinib to Inhibit JAK/STAT Signaling in Refractory Colorectal Cancer Terminated Colorectal Cancer NCT02277093
Pacritinib Before Transplant for Myeloproliferative Neoplasms (MPN) Terminated Myeloproliferative Diseases NCT02410551
Pacritinib in Combination With Low Dose Decitabine in Intermediate-High Risk Myelofibrosis or Myeloproliferative Neoplasm (MPN)/Myelodysplastic Syndrome (MDS) Withdrawn Chronic Myelomonocytic Leukemia|Juvenile Myelomonocytic Leukemia|Atypical Chronic Myeloid Leukemia|Myeloproliferative Neoplasm|Myelodysplastic Syndromes|Myelofibrosis NCT02564536
Pacritinib for Patients With Lower-Risk Myelodysplastic Syndromes (MDS) Terminated Leukemia NCT02469415
PK of Pacritinib in Patients With Mild, Moderate, Severe Renal Impairment and ESRD Compared to Healthy Subjects Completed Myelofibrosis NCT02807077
Study to Assess the Relative Bioavailability of Pacritinib Following Oral Administration as Capsule and Solution Formulations in Healthy Subjects Completed Healthy Subjects NCT02808455
A Phase I/II GVHD Prevention Trial Combining Pacritinib With Sirolimus-Based Immune Suppression Recruiting Graft Vs Host Disease|GVHD NCT02891603
A Phase II Non-Controlled, Open-Label, Efficacy, Safety, Pharmacokinetic, and Pharmacodynamic Study of Pacritinib in Myelofibrosis Withdrawn Primary Myelofibrosis NCT02584777
Pacritinib and Chemotherapy in Treating Patients With Acute Myeloid Leukemia and FLT3 Mutations Completed Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia NCT02323607
Pacritinib in Patients With Endothelial Growth Factor (EGFR) Mutant Non-small Cell Lung Cancer (NSCLC) After EGFR Tyrosine Kinase Inhibitor (TKI) Terminated Non-Small Cell Lung Cancer|Nonsmall Cell Lung Cancer|Carcinoma, Non-Small-Cell Lung NCT02342353
To Assess the Bioequivalence of Two Pacritinib Drug Product Formulations and FMI Formulation Following Oral Administration in Healthy Subjects Completed Healthy NCT02823171
To Evaluate the Cardiac Safety and PK Following a Single Oral Dose Administration of Pacritinib in Healthy Subjects Completed Healthy Subjects NCT02807207

References

Publication DOI Pubmed PMCID
The JAK2/STAT3 inhibitor pacritinib effectively inhibits patient-derived GBM brain tumor initiating cells in vitro and when used in combination with temozolomide increases survival in an orthotopic xenograft model. PloS one Katharine Victoria Jensen, Orsolya Cseh, Ahmed Aman, Samuel Weiss, Hema Artee Luchman, 12, 12, None, 2017-12-18, 10.1371/journal.pone.0189670 10.1371/journal.pone.0189670 29253028 PMC5734728

Vendors

Company Lnk to product
Selleckchem https://www.selleckchem.com/products/pacritinib-sb1518.html
MedChemExpress https://www.medchemexpress.com/pacritinib.html
Caymanchemicals https://www.caymanchem.com/product/16709/pacritinib

Filter data

Compound Pacritinib
Experiment types Alamar Blue assay, Average survival, Western Blot
Concentrations 0.20, 0.50, 0.62, 0.92, 0.99, 1.00, 1.01, 1.03, 1.08, 1.22, 1.26, 1.33, 1.36, 1.66, 10.00, 100.00, 2.00, 3.00, 5.00
Cell lines BT12, BT124, BT143, BT147, BT189, BT48, BT50, BT53, BT67, BT68, BT69
Organisms Homo sapiens
Animal models
STAT proteins STAT3, p-STAT3 (Y705)
Other AKT, Actin, PARP, p-AKT S473, p-p44/42 MAPK, p44/42 MAPK

Experiments

Compound Experiment type Investigated event Concentration Cell line Organism Animal model Stat protein Details
Pacritinib Alamar Blue assay Infuence on cell viability 1.66 µM BT12 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.03 µM BT48 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 0.62 µM BT50 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 0.92 µM BT53 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.08 µM BT67 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.22 µM BT68 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.26 µM BT69 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.33 µM BT124 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.36 µM BT143 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 0.99 µM BT147 Homo sapiens
Pacritinib Alamar Blue assay Infuence on cell viability 1.01 µM BT189 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT69 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 3.00 µM BT69 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 3.00 µM BT69 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT69 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens p-STAT3 (Y705)
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens STAT3
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT147 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.20 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 0.50 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 1.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 2.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 3.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 5.00 µM BT53 Homo sapiens
Pacritinib Western Blot Influence on protein activity 10.00 µM BT53 Homo sapiens
Pacritinib Average survival Influence on survival 100.00 mg/kg BT147 Homo sapiens
Pacritinib Average survival Influence on survival 100.00 mg/kg BT53 Homo sapiens
Pacritinib Average survival Influence on survival in tresence of TMZ 100.00 mg/kg BT147 Homo sapiens
Pacritinib Average survival Influence on survival in tresence of TMZ 100.00 mg/kg BT53 Homo sapiens