Pacritinib (SB1518)

For research use only.

Catalog No.S8057

6 publications

Pacritinib (SB1518) Chemical Structure

CAS No. 937272-79-2

Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.

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Selleck's Pacritinib (SB1518) has been cited by 6 publications

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  • Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting

    Clin Cancer Res, 2016, 22(24):6118-6128. Pacritinib (SB1518) purchased from Selleck.

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Biological Activity

Description Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.
Features Dual JAK2/FLT3 inhibitor that has progressed to Phase III clinical trials for treatment of Myelofibrosis.
Targets
FLT3 (D835Y) [1]
(Cell-free assay)
JAK2 (V617F) [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
6 nM 19 nM 22 nM 23 nM 50 nM
In vitro

Pacritinib is a potent inhibitor of both wild-type JAK2 and JAK2V617F mutant (IC50= 19 nM) that is present in high frequencies among patients with MPD. Relative to JAK2, Pacritinib is two-fold less potent against TYK2 (IC50= 50 nM), 23-fold less potent against JAK3 (IC50= 520 nM) and 56-fold less potent against JAK1 (IC50= 1280 nM). Pacritinib effectively permeates cells to modulate signaling pathways downstream of JAK2, whether agonist activated or mutationally activated. Pacritinib induces apoptosis, cell cycle arrest and antiproliferative effects in JAK2WT- and JAK2V617F-dependent cells. Pacritinib inhibits cell proliferation of Karpas 1106P and Ba/F3-JAK2V617F with IC50 of 348 and 160 nM, respectively. Pacritinib inhibits endogenous colony growth derived from erythroid and myeloid progenitors with IC50 of 63 and 53 nM , respectively. [1] SB1518 also inhibits FLT3 and its mutant FLT3-D835Y(IC50= 6 nM ). Pacritinib inhibits FLT3 phosphorylation and downstream STAT, MAPK and PI3K signaling in FLT3-internal-tandem duplication (ITD), FLT3-wt cells and primary AML blast cells. Pacritinib treatment leads to a dose-dependent decrease of pFLT3, pSTAT5, pERK1/2 and pAkt in FLT3-ITD harboring MV4-11 cells with IC50 of 80, 40, 33 and 29 nM , respectively. Treatment of the primary AML blast cells with Pacritinib for 3 h leads to a dose-dependent decrease of pFLT3, pSTAT3 and pSTAT5 with an IC50 below 0.5 μM. Pacritinib induces apoptosis, cell cycle arrest and anti-proliferative effects in FLT3-mutant and FLT3-wt cells. Pacritinib inhibits cell proliferation of FLT3-ITD-harboring cells MV4-11 and primary AML blast cells with IC50s of 47 nM and 0.19-1.3 μM, respectively. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HL60 MkjmRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3nKOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczygTWM2OCB;IEGuO|gh|ryPLh?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
AC10 M4e3VGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHjxWZkzPCCqcoO= Mmq2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRWMyOCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjCyOEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFIvODJizszNMi=> Mn;1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
TAMH Mn3WR5l1d3SxeHnjbZR6KGG|c3H5 Mn31NlQhcHK| MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBVSU2KIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFI1KGi{czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCLQ{WwJF0hOy54ODFOwG0v NI\VfpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
KMS-12-BM M3rRSGZ2dmO2aX;uJIF{e2G7 NUjzVGpyOiC3TR?= NYfhc2t6OyCqcoO= M1rLVGlvcGmkaYTpc44hd2ZiSlHLNkBqdiCLTD22MZN1cW23bHH0[YQhcHWvYX6gT21UNTF{LVLNJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCCWWUewOUBz\XOrZIXlJIF1KDJidV2gdJJmfHKnYYTl[EBnd3JiMzDodpMh\m:ubH;3[YQh[nliSVytOkB{fGmvdXzheIlwdiCkeTDpcY12dm:kbH;0JI1mfGixZB?= NGXhW|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
MOLM14 MoPpSpVv[3Srb36gZZN{[Xl? NY\3dXpYOC5zIIXN MkXUN{BpenN? Mn7DTY5pcWKrdHnvckBw\iCMQVuyJIlvKEmOLU[td5RqdXWuYYTl[EBpfW2jbjDNU2xOOTRiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JHR[PzB3IILld4llfWViYYSgNE4yKHWPIIDy[ZRz\WG2ZXSg[o9zKDNiaILzJIZwdGyxd3XkJIJ6KEmOLU[gd5RqdXWuYYTpc44h[nliaX3teY5w[myxdDDt[ZRpd2R? NE\jVGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
HEL 92.1.7 NITp[ndHfW6ldHnvckBie3OjeR?= NUXjRZZsOSCqch?= NEnDfYdKdmS3Y4Tpc44hd2ZiSlHLNkBXPjF5RjDteZRidnRicHjvd5Bpd3K7bHH0bY9vKGG2IGmxNFA4NzhicnXzbYR2\XNiaX6gTGVNKDl{LkGuO{Bk\WyuczDh[pRmeiBzIHjyJIJ6KGmvbYXuc4Jtd3RibXX0bI9l M33xZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=

... Click to View More Cell Line Experimental Data

In vivo Pacritinib administrated at 150 mg/kg p.o. q.d. to JAK2V617F-dependent xenograft model, significantly ameliorates splenomegaly and hepatomegaly symptoms, with 60% normalization of spleen weight and 92% normalization of liver weight and is well tolerated without significant weight loss or any hematological toxicities, including thrombocytopenia and anemia. Pacritinib induces dose-dependent inhibition of tumor growth of JAK2V617F-dependent SET-2 xenograft model (40% for 75 mg/kg and 61% for 150 mg/kg). [1] Pacritinib is efficacious in FLT3-ITD-bearing MV4-11 xenograft models. Pacritinib treated once daily for 21 consecutive days, induces dose-dependent inhibition of tumor growth (38% for 25 mg/kg, 92% for 50 mg/kg and 121% for 100 mg/kg). Complete regression is observed in 3/10 and 8/8 mice for the 50 and 100 mg/kg/day groups, respectively. [2]

Protocol

Kinase Assay:[1]
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kinase activity assays:

All assays are carried out in 384-well white microtiter plates. Compounds are 4-fold serially diluted in 8 steps, starting from 10 μM. The reaction mixture consisted of 25 μL assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 5 mM β-glycerol phosphate). For FLT3 assays, the reaction contains 2.0 μg/mL FLT3 enzyme, 5 μM of poly(Glu,Tyr) substrate and 4 μM of ATP. For JAK1 assays, the reaction contains 2.5 μg/mL of JAK1 enzyme, 10 μM of poly(Glu,Ala,Tyr) substrate and 1.0 μM of ATP. For JAK2 assays, the reaction contained 0.35 μg/mL of JAK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. For JAK3 assays, the reaction contained 3.5 μg/mL of JAK3 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 6.0 μM of ATP. For TYK2 assays, the reaction contained 2.5 μg/mL of TYK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. The reaction is incubated at room temperature for 2 h prior to addition of 13 μL PKLight® detection reagent. After 10 min incubation luminescent signals are read on a multi-label plate reader.
Cell Research:[1]
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  • Cell lines: Karpas 1106P cells
  • Concentrations: ~10 μM
  • Incubation Time: 2 days
  • Method: Cells are seeded at 30-50% confluency in 96-well plates and are treated with different concentrations of compounds (in triplicate) for 48 h. Cell viability is monitored using the CellTiter-Glo assay.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Human megakaryoblastic leukemia xenografts SET-2
  • Dosages: 150 mg/kg
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 11 mg/mL warmed (23.27 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.58
Formula

C28H32N4O3

CAS No. 937272-79-2
Storage powder
in solvent
Synonyms N/A
Smiles C1CCN(C1)CCOC2=C3COCC=CCOCC4=CC(=CC=C4)C5=NC(=NC=C5)NC(=C3)C=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04520269 Recruiting Drug: Pacritinib Breast Cancer National University Hospital Singapore July 13 2020 Phase 1|Phase 2
NCT03165734 Recruiting Drug: Pacritinib|Drug: Physician''s Choice medications Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis CTI BioPharma|PSI CRO AG June 26 2017 Phase 3
NCT02677948 Withdrawn Drug: Pacritinib|Drug: Ibrutinib Chronic Lymphocytic Leukemia|Lymphoma Small Lymphocytic University of Michigan Rogel Cancer Center October 2016 Phase 1|Phase 2
NCT02584777 Withdrawn Biological: Pacritinib Primary Myelofibrosis Baxalta now part of Shire|CTI BioPharma|Shire November 2015 Phase 2
NCT02765724 Completed Drug: Pacritinib Myelofibrosis CTI BioPharma|SGS S.A. January 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID