Pacritinib hydrochloride
Based on 19 publication(s) in Google Scholar
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF).
For research use only. We do not sell to patients.
- CAS No.: 1228923-43-0
- Formula: C28H32N4O3.xClH
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Pacritinib hydrochloride
More- Nat Med. 2017 Nov;23(11):1319-1330. [Abstract]
- Science. 2026 Feb 5;391(6785):eadz4075. [Abstract]
- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]
- Nat Commun. 2021 Jul 21;12(1):4441. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Death Dis. 2021 Dec 20;13(1):16. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Inflamm Res. 2020 Jan;69(1):51-62. [Abstract]
- Drug Des Devel Ther. 2018 Apr 30:12:1009-1017. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- PLoS Pathog. 2025 Jun 23;21(6):e1013281. [Abstract]
- PLoS Genet. 2024 May 28;20(5):e1011293. [Abstract]
- BMJ Open Ophthalmol. 2026 Jan 12;11(1):e002307. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- bioRxiv. 2025 June 03.
- bioRxiv. 2025 February 21.
- Patent. US20220323444A1.
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WB
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RT-PCR
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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WB
Biological Activity
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JAK2V617F 19 nM (IC50) |
JAK2wt 23 nM (IC50) |
Tyk2 50 nM (IC50) |
JAK3 520 nM (IC50) |
JAK1 1280 nM (IC50) |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1228923-43-0
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Formula C28H32N4O3.xClH
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SMILES
[H]Cl.C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1.[x]
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Synonyms
SB1518 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (19)
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Journal Impact Factor
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Most Recent
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Nat Med
Chromosome 1q21.3 amplification is a trackable biomarker and actionable target for breast cancer recurrence. [Abstract]2017 Nov;23(11):1319-1330. PMID: 28967919
Pacritinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Nov;23(11):1319-1330. [Abstract]
Pacritinib effectively disrupts the S100A7/8/9–IRAK1 feedback loop to inhibit tumorsphere growth. Representative western blot (n=2) showing inhibition of phosphorylated IRAK1 and phosphorylated JAK2 (pJAK2) within 6 h of Pacritinib treatment in MB468 and MB231 cells. Actin is used as a loading control.
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Science
2026 Feb 5;391(6785):eadz4075. PMID: 41643022 -
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Nat Commun
Genotoxic stress and viral infection induce transient expression of APOBEC3A and pro-inflammatory genes through two distinct pathways. [Abstract]2021 Aug 13;12(1):4917. PMID: 34389714
Pacritinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]
Pacritinib (0.25-1 µM; 6 h) treatment caused inhibition of phosphorylated IRAK1 and phosphorylated JAK2 (pJAK2) in MB468 and MB231 cells.
Pacritinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]
Real-time PCR analysis of S100A7, S100A8, and S100A9 gene expression after Pacritinib (0.25-1 µM; 24 h) treatment in MB468 cells.
Pacritinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]
NOD-SCID mice bearing MB231 and HCC70 tumors were treated with pacritinib (50, 100, or 150 mg/kg; p.o.; once daily for 21 d). Pacritinib treatment in different doses resulted in substantial inhibition of tumor growth for HCC70 xenograft tumors but had no obvious effect on the growth of MB231 xenografts.
Pacritinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]
Growth curve of tumorspheres from ER-positive and ER-negative breast cancer cell lines treated with increasing doses of Pacritinib (0.25-5 µM). Pacritinib treatment was more effective in impairment of tumorsphere growth in cancer cell lines positive for 1q21.3 amplification than in cell lines without amplification.
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Nat Commun
Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer. [Abstract]2021 Jul 21;12(1):4441. PMID: 34290255 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Death Dis
Colorectal cancer-associated fibroblasts promote metastasis by up-regulating LRG1 through stromal IL-6/STAT3 signaling. [Abstract]2021 Dec 20;13(1):16. PMID: 34930899 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Inflamm Res
Potent repression of C-reactive protein (CRP) expression by the JAK1/2 inhibitor ruxolitinib in inflammatory human hepatocytes. [Abstract]2020 Jan;69(1):51-62. PMID: 31654094 -
Drug Des Devel Ther
Advances in the drug therapies of acute myeloid leukemia (except acute wpromyelocytic leukemia). [Abstract]2018 Apr 30:12:1009-1017. PMID: 29750014 -
Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
PLoS Pathog
Kaposi sarcoma-associated herpesvirus cooperates with Epstein-Barr virus to co-transform a small set of human B cells oncogenically. [Abstract]2025 Jun 23;21(6):e1013281. PMID: 40549805 -
PLoS Genet
Her2 amplification, Rel-A, and Bach1 can influence APOBEC3A expression in breast cancer cells. [Abstract]2024 May 28;20(5):e1011293. PMID: 38805570 -
BMJ Open Ophthalmol
Impact of anticancer drugs on human Tenon's fibroblast proliferation: implications for glaucoma surgery. [Abstract]2026 Jan 12;11(1):e002307. PMID: 41526033 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
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Purity & Documentation
References
[1]. Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25(11):1751-9. [Content Brief]
[2]. Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 2011 Nov;1(11):e44. [Content Brief]
[3]. Komrokji RS, et al. Results of a phase 2 study of pacritinib (SB1518), a JAK2/JAK2(V617F) inhibitor, in patients with myelofibrosis. Blood. 2015 Apr 23;125(17):2649-55. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)