Cat. No.: HY-16379A

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Pacritinib hydrochloride

Name: Pacritinib hydrochloride
Brand: MedChemExpress
SKU: HY-16379A
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(Synonyms: SB1518 hydrochloride)

20 Cited Publications

Customer Review

Based on 20 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

CAS No.: 1228923-43-0
Formula: C₂₈H₃₂N₄O₃.xClH

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (295 KB)

Pacritinib hydrochloride Chemical Structure

CAS No.: 1228923-43-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (20)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

JAK2

23 nM (IC₅₀)

FLT3

22 nM (IC₅₀)

STAT5

ERK1

ERK2

All JAK Isoforms :

All STAT Isoforms :

All ERK Isoforms :

All Akt Isoforms :

In Vitro

Anti-cancerApoptosisInnate ImmunityAdaptive ImmunityCytokines & ChemokinesImmune Tolerance & ImmunosuppressionOthers

Anti-cancer

Pacritinib (up to 10 μM; 48 h) hydrochloride inhibits proliferation of AML cell lines, with IC₅₀ values of 47 nM in MV4-11, 67 nM in MOLM-13, 220 nM in SET-2, and 930 nM in RS4;11^[1].
Pacritinib (8-1000 nM; 3 h) hydrochloride inhibits FLT3 autophosphorylation and downstream STAT5, MAPK, and PI3K signaling in FLT3-ITD and FLT3-wt AML cell lines, with pSTAT5 IC₅₀ values of 40 nM in MV4-11, 20 nM in MOLM-13, and 8 nM in RS4;11^[1].
Pacritinib hydrochloride inhibits the proliferation of leukemia and lymphoma cell lines dependent on JAK2 or FLT3 activation, with an IC₅₀ of 35-240 nM^[4].
Pacritinib hydrochloride inhibits JAK/STAT signaling and proliferation in cancer cell lines, including Karpas 1106P and Karpas1160, with an IC₅₀ of 110 ng/mL for Karpas1160 proliferation^[7].

Apoptosis

Pacritinib (0.5 nM-10 μM; 16 h) hydrochloride induces caspase-3/7 activation in MV4-11 cells with an EC₅₀ of 0.96 μM^[1].
Pacritinib (0.03-0.15 μM; 48-72 h) hydrochloride dose-dependently increases early and late apoptosis in MV4-11 cells without inducing necrosis^[1].
Pacritinib hydrochloride combined with Pracinostat (HY-13322) completely eliminates JAK2 autophosphorylation in SET-2 cells and enhances apoptosis markers in SET-2, HEL92.1.7, MV4-11, and MOLM-13 cells^[2].

Innate Immunity

Adaptive Immunity

Cytokines & Chemokines

Pacritinib hydrochloride combined with Sirolimus (HY-10219) inhibits the production of IFNγ, IL13, and GMCSF in DC alloantigen-stimulated human T cells^[5].

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Anti-cancer

Pacritinib (10 µM; 5-7 days) hydrochloride inhibits TH1, TH17, and Treg differentiation and CFSE-based T cell proliferation in MNC cultures from MPN samples and normal controls^[6].

Others

Pacritinib hydrochloride has comparable potency against JAK2 and FLT3 in cell-free kinase assays, with IC₅₀ values of 23 nM and 22 nM, respectively^[1].
Pacritinib (1 μM; 24 h) hydrochloride reduces fibrosis marker expression and proliferation in primary mouse wild-type and SM22Cre⁺-Jak2f/f HSCs as well as LX-2 and TWNT-4 HSCs, with JAK2-dependent effects in mouse HSCs^[3].
Pacritinib hydrochloride inhibits JAK2, JAK2 V617F, FLT3, and FLT3 D835Y with IC₅₀ values of 6-22 nM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

AML cell lines, including SET-2, MV4-11, MOLM-13, RS4;11, and other AML-derived lines
Concentration:

up to 10 μM
Incubation Time:

48 h
Result:

Showed the highest potency in FAB M5 subtype lines (THP-1, MV4-11, and MOLM-13).
SET-2 (JAK2V617F) IC₅₀ = 0.22 μM; MV4-11 IC₅₀ = 47 nM; MOLM-13 IC₅₀ = 67 nM; RS4;11 IC₅₀ = 930 nM; MV4-11-P IC₅₀ = 153 nM; MV4-11-R IC₅₀ = 434 nM, a 2.9-fold difference between parental and resistant cells.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.5 nM-10 μM
Incubation Time:

16 h
Result:

Dose-dependently activated caspase-3/7, with an EC₅₀ of 0.96 μM.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.03 and 0.15 μM
Incubation Time:

48 h and 72 h
Result:

At 48 h, 0.03 mM increased early and late apoptotic cells to 24.50% and 5.58%, respectively; 0.15 mM increased them to 39.39% and 20.83%.
At 72 h, 0.03 mM increased early and late apoptotic cells to 22.69% and 3.74%; 0.15 mM increased them to 58.69% and 15.10%.
No necrosis induction was observed.

Western Blot Analysis^[1]

Cell Line:

MV4-11, MOLM-13, and RS4;11 cells
Concentration:

8, 40, 200, 1000 nM
Incubation Time:

3 h (MOLM-13 and RS4;11 plus 10 ng/mL FLT3 ligand for 3 min)
Result:

In MV4-11, dose-dependent decreases occurred in pFLT3, pSTAT5, pERK1/2, and pAkt with IC₅₀ values of 80, 40, 33, and 29 nM, respectively.
In MOLM-13, IC₅₀ values were 180 nM for pFLT3 and 20 nM for pSTAT5.
In RS4;11, IC₅₀ values were 600 nM for pFLT3 and 8 nM for pSTAT5.

In Vivo

Anti-cancerCytokines & ChemokinesAdaptive ImmunityImmune Tolerance & ImmunosuppressionOthers

Anti-cancer

Pacritinib (Pacritinib hydrochloride; 25-100 mg/kg; once daily; for 21 consecutive days) hydrochloride produces dose-dependent tumor growth inhibition and complete regression in the MV4-11 AML xenograft model^[1].
Pacritinib (Pacritinib hydrochloride; 150 mg/kg; oral; twice daily; for 7 consecutive days) hydrochloride inhibits MOLM-13 tumor growth and reduces lung metastasis in the MOLM-13 AML xenograft model in vivo^[1].
Pacritinib (oral) hydrochloride demonstrates target inhibition and antitumor activity in the MV4-11 leukemia model in nude mice^[4].

Anti-cancer

Cytokines & Chemokines

Pacritinib (150 mg/kg; oral; twice daily; 19 days (d0-d18)) hydrochloride inhibits SET-2 AML xenograft tumor growth, reduces pSTAT5 and the incidence of lymph node metastasis, and normalizes plasma levels of IL-6, IP-10, and KC^[2].

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Pacritinib (50 mg/kg; 14 days) hydrochloride reduces pathogenic CD4⁺ pSTAT3⁺ and Th1/Th17 cells and preserves Tregs in xenogeneic GVHD NSG mice, and PAC/SIR (50 mg/kg plus sirolimus; 14 days) improves survival and GVHD scores^[5].

Others

Pacritinib (65 μg/kg; intravenous injection; twice weekly; 4 weeks) hydrochloride attenuates liver injury and fibrosis in the CCl₄/ethanol-induced ASH mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (BALB/cOlaHsd-Foxn1nu; female; athymic; 9-16 weeks of age at tumor implantation)^[1]
Dosage:

25 mg/kg, 50 mg/kg, and 100 mg/kg (efficacy); 150 mg/kg (target engagement)
Administration:

oral; once daily; 21 consecutive days; single dose (target engagement)
Result:

Induced dose-dependent tumor growth inhibition: 38% at 25 mg/kg, 92% at 50 mg/kg, and 121% at 100 mg/kg.
Complete regression was observed in 3/10 mice at 50 mg/kg/day and 8/8 mice at 100 mg/kg/day.
A single 150 mg/kg dose blocked FLT3 and downstream signaling in tumor tissues at 2 and 4 h; pSTAT5 (Y694) was decreased in tumor lysates at 2 and 4 h compared with vehicle.

Animal Model:

C.B-17/IcrHan (Hsd-Prkdcscid; female; severe combined immunodeficiency)^[1]
Dosage:

150 mg/kg (efficacy); 150 mg/kg (target engagement)
Administration:

oral; b.i.d.; 7 consecutive days (methods state 8 consecutive days); single dose (target engagement)
Result:

Dosing resulted in 83% tumor growth inhibition after 7 days of dosing.
Metastatic incidence (mostly in the lungs) was reduced from 0.83 to 0.33 in the high-dose pacritinib group.
A single 150 mg/kg dose blocked FLT3 and downstream signaling at 3 h; in tumor lysates, pSTAT5 (Y694) was fully inhibited 3 h after the last dose on day 7.

Animal Model:

C.B-17.Cg-PrkdcscidLystbg/Crl (female, 9 weeks old)^[2]
Dosage:

150 mg/kg (doses refer to free base)
Administration:

p.o. gavage; twice daily; for 19 days (d0-d18)
Result:

Led to 61% tumor growth inhibition based on tumor volume and 47% tumor growth inhibition based on tumor weight.
pSTAT5 levels in tumors were decreased by about 50% after chronic monotherapy.
No lymph node metastases were observed in mice dosed with pacritinib alone.
Plasma MCP-1 levels in tumor-bearing mice were reduced by 10% after pacritinib monotherapy; IL-6, IP-10, and KC were normalized.

Animal Model:

C57BL/6J (wild-type, male, 10-12 weeks old)^[3]
Dosage:

65 μg/kg body weight
Administration:

i.v. injection; twice per week; starting 3 weeks after first CCl4 injection for 4 weeks
Result:

Reduced serum ALT levels.
Reduced serum AST levels.
Improved liver parenchyma by H&E staining.
Decreased Sirius red collagen staining.
α-SMA immunostaining showed a trend toward reduction.
Collagen-1 and p-moesin protein levels were reduced.
Col1a1 mRNA expression showed a trend toward reduction, while Acta2 and Tgfb showed no changes.
No changes were observed in steatosis markers, oil red O staining, hepatic triglyceride content, or liver-to-body weight ratio.

Animal Model:

NSG (male or female, age 6 to 24 weeks old)^[5]
Dosage:

50 mg/kg (PAC); 50 mg/kg plus sirolimus (PAC/SIR)
Administration:

for 14 days
Result:

Decreased the frequency of CD4+, pSTAT3+ human T cells in mouse spleens at day 14.
Increased the amount of Tregs in mouse spleen at day 14.
Improved survival from xenogeneic GVHD compared with either inhibitor alone.
Reduced GVHD scores.
Decreased the frequency of CD4+, pSTAT3+ human T cells at day 14.
Decreased CD4+, pS6+ T cells at day 14.
Decreased both CD4+, pSTAT3+ and pS6+ T cells.
Decreased the frequency of pathogenic Th1 cells in the spleen at day 14.
Decreased human Th17 cells at day 14.
Had similar Th2 cell frequency.
Did not increase Treg frequency in mice transplanted with standard human PBMCs.
In mice transplanted with Treg-depleted PBMCs, PAC/SIR produced more human Tregs at day 14 in mouse spleens compared with sirolimus.
PAC/SIR-treated mice retained high frequencies of CD4+, pH3ser10+ T cells compared with controls.

Related Protocols :

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS No. 1228923-43-0
Formula C₂₈H₃₂N₄O₃.xClH
SMILES

[H]Cl.C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1.[x]
Synonyms

SB1518 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (20)

All WBRT-PCRIn Vivo Efficacy StudyCell Proliferation/Viability Assay

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Journal Impact Factor

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.
Science

Antifibrotic drug finerenone restores fertility in premature ovarian insufficiency. [Abstract]

2026 Feb 5;391(6785):eadz4075. PMID: 41643022
Science

The target landscape of clinical kinase drugs. [Abstract]

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.
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 Cancer Ther

2026 Jul 14. PMID: 42442343
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

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

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
bioRxiv

2025 June 03.
bioRxiv

2025 February 21.
Patent

US20220323444A1.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (295 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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.

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Pacritinib hydrochloride

20 Cited Publications

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Pacritinib hydrochloride

Publications Citing Use of MedChemExpress (MCE) Pacritinib hydrochloride

All JAK Isoforms

All STAT Isoforms

All ERK Isoforms

All Akt Isoforms