1228923-43-0
Chemical Structure
Pacritinib hydrochloride
Synonym(s): SB1518 hydrochloride
- CAS No.: 1228923-43-0
- Formula:C28H32N4O3.xClH
- Molecular Weight:N/A
SMILES: [H]Cl.C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1.[x]
Biological Activity: Pacritinib hydrochloride (SB1518 hydrochloride) is an orally active, selective JAK2/FLT3 inhibitor with IC50 values of 23 nM and 22 nM, respectively. Pacritinib hydrochloride inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib hydrochloride normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib hydrochloride can be used in research on acute myeloid leukemia, myeloproliferative neoplasms, leukemia/lymphoma, GVHD, and alcoholic/non-alcoholic liver fibrosis[1][2][3][4][5][6][7].
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Pacritinib hydrochloride | Pacritinib hydrochloride (SB1518 hydrochloride) is an orally active, selective JAK2/FLT3 inhibitor with IC50 values of 23 nM and 22 nM, respectively. Pacritinib hydrochloride inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib hydrochloride normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib hydrochloride can be used in research on acute myeloid leukemia, myeloproliferative neoplasms, leukemia/lymphoma, GVHD, and alcoholic/non-alcoholic liver fibrosis. | |||||||||||||||||||||
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References
- [1]. Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood cancer journal. 2011 Nov;1(11):e44. [Content Brief]
- [2]. Novotny-Diermayr V, et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood cancer journal. 2012 May;2(5):e69. [Content Brief]
- [3]. Torres S, et al. Janus kinase 2 inhibition by pacritinib as potential therapeutic target for liver fibrosis. Hepatology (Baltimore, Md.). 2023 Apr 01;77(4):1228-1240.
- [4]. Hart S, et al. Pharmacodynamic (PD) Biomarker Assay Validation for SB1518, a Novel Oral JAK2 Inhibitor in Phase 1 Clinical Trials for Advanced Leukemias, Myeloproliferative Diseases and Lymphoma. Blood. 2009 Nov 20;114(22):1888.
- [5]. Pidala J, et al. Pacritinib Combined with Sirolimus and Low-Dose Tacrolimus for GVHD Prevention after Allogeneic Hematopoietic Cell Transplantation: Preclinical and Phase I Trial Results. Clinical cancer research : an official journal of the American Association for Cancer Research. 2021 May 15;27(10):2712-2722.
- [6]. Chen C, et al. Comparison of Ruxolitinib, Momelotinib, and Pacritinib in the Inhibition of Immune Differentiation and Proliferation of T Cells in Myeloproliferative Neoplasm. Blood. 2015 Dec 3;126(23):5203.
- [7]. Younes A, et al. Phase I study of a novel oral Janus kinase 2 inhibitor, SB1518, in patients with relapsed lymphoma: evidence of clinical and biologic activity in multiple lymphoma subtypes. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2012 Nov 20;30(33):4161-7.
