937272-79-2
Chemical Structure
Pacritinib
Synonym(s): SB1518
- CAS No.: 937272-79-2
- Formula:C28H32N4O3
- Molecular Weight:472.58
IUPAC Name: (22Z,23E,8E)-44-(2-(pyrrolidin-1-yl)ethoxy)-21,22-dihydro-6,11-dioxa-3-aza-2(4,2)-pyrimidina-1,4(1,3)-dibenzenacyclododecaphan-8-ene
InChIKey: HWXVIOGONBBTBY-ONEGZZNKSA-N
SMILES: C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1
Biological Activity: Pacritinib (SB1518) is an orally active, selective JAK2/FLT3 inhibitor with IC50 values of 23 nM and 22 nM, respectively. Pacritinib inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Pacritinib | 99.88% | Pacritinib (SB1518) is an orally active, selective JAK2/FLT3 inhibitor with IC50 values of 23 nM and 22 nM, respectively. Pacritinib inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib can be used in research on acute myeloid leukemia, myeloproliferative neoplasms, leukemia/lymphoma, GVHD, and alcoholic/non-alcoholic liver fibrosis. | ||||||||||||||||||||
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Pacritinib (Standard) | ≥98% | Pacritinib (Standard) (SB1518 (Standard)) is the analytical standard of Pacritinib (HY-16379). This product is intended for research and analytical applications. Pacritinib (SB1518) is an orally active, selective JAK2/FLT3 inhibitor with IC50 values of 23 nM and 22 nM, respectively. Pacritinib inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib can be used in research on acute myeloid leukemia, myeloproliferative neoplasms, leukemia/lymphoma, GVHD, and alcoholic/non-alcoholic liver fibrosis. | ||||||||||||||||||||
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Pacritinib-d4 | 98.42% | Pacritinib-d4 (SB1518-d4) is the deuterated-labeled Pacritinib (HY-16379). Pacritinib (SB1518) is an orally active, selective JAK2/FLT3 inhibitor with IC50 values of 23 nM and 22 nM, respectively. Pacritinib inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib 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.
