Parsaclisib (INCB050465) Hydrochloride

Catalog No.S8779 Synonyms: IBI376

For research use only.

Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

Parsaclisib (INCB050465) Hydrochloride Chemical Structure

CAS No. 1995889-48-9

Purity & Quality Control

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Biological Activity

Description Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
Targets
PI3Kδ [1]
(in biochemical assay)
1 nM
In vitro

Parsaclisib inhibits proliferation of MCL and DLBCL cell lines, and anti-IgM-induced pAKT (Ser473) in the Ramos Burkitt’s lymphoma cell line. <sup><a class="sref" href="#s_ref">[1]</a></sup>

In vivo

Parsaclisib inhibits tumor growth in the BALB/c mice bearing the A20 murine lymphoma cells, by reducing the number of Tregs in the tumors and spleens of treated mice.<sup><a class="sref" href="#s_ref">[1]</a></sup>

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MCL Cell Lines, DLBCL Cell Lines, Ramos Burkitt’s lymphoma cell lines
  • Concentrations: --
  • Incubation Time: 2 h
  • Method:

    The cells are first serum starved in 0.2% fetal bovine serum overnight, followed by treatment with parsaclisib for 2 hours, and then stimulated with anti-IgM (4 μg/ml) or C5a (10 μg/ml) for 10 minutes. And then cells are stained with an anti-pAKT (Ser473) antibody and analyzed with Western analysis.

Animal Research:

[1]

  • Animal Models: B cell lymphoma model Female BALB/c mice (5-9 weeks) inoculated with A20 cells
  • Dosages: 10 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 94 mg/mL
(200.28 mM)
Water Insoluble
Ethanol ''94 mg/mL

Chemical Information

Molecular Weight 469.34
Formula

C20H23Cl2FN6O2

CAS No. 1995889-48-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=C(C(=C(C=C1C(C)N2C3=NC=NC(=C3C(=N2)C)N)Cl)F)C4CC(=O)NC4

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04774068 Recruiting Drug: Parsaclisib|Drug: Romidepsin Recurrent Anaplastic Large Cell Lymphoma|Recurrent Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Recurrent Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Recurrent Transformed Mycosis Fungoides|Refractory Anaplastic Large Cell Lymphoma|Refractory Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Refractory Primary Cutaneous T-Cell Non-Hodgkin Lymphoma|Refractory Transformed Mycosis Fungoides|T-Cell Non-Hodgkin Lymphoma Ohio State University Comprehensive Cancer Center September 1 2021 Phase 1
NCT04831996 Recruiting Drug: parsaclisib Advanced Malignancies Incyte Corporation May 4 2021 Phase 1
NCT04831944 Recruiting Drug: parsaclisib Advanced Malignancies Incyte Corporation March 29 2021 Phase 1
NCT04142554 Withdrawn Drug: Parsaclisib Breast Cancer|Breast Neoplasms|Triple Negative Breast Cancer|HER2-positive Breast Cancer UNC Lineberger Comprehensive Cancer Center|Incyte Corporation June 1 2020 Phase 1
NCT04298879 Recruiting Drug: IBI376 Indolent Non-hodgkin Lymphoma Innovent Biologics (Suzhou) Co. Ltd. April 7 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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