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Parsaclisib hydrochloride (Synonyms: INCB050465 hydrochloride)

Cat. No.: HY-109068A Purity: 98.74%
Handling Instructions

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies.

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

Parsaclisib hydrochloride Chemical Structure

Parsaclisib hydrochloride Chemical Structure

CAS No. : 1995889-48-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 5679 In-stock
Estimated Time of Arrival: December 31
5 mg USD 5500 In-stock
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10 mg USD 8500 In-stock
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25 mg USD 17500 In-stock
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50 mg USD 27500 In-stock
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100 mg USD 39500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies[1][2][3].

IC50 & Target[1]

PI3Kδ

1 nM (IC50)

In Vitro

Parsaclisib (0.1-3000 nM; 4 d) inhibits proliferation of MCL and DLBCL cell lines[2].
Parsaclisib (0.1-1000 nM; 2 h) inhibits anti-IgM-induced pAKT (Ser473) in the Ramos Burkitt’s lymphoma cell line, with an IC50 of 1 nM[2].
Parsaclisib inhibits the proliferation of human, dog, rat, and mouse primary B cells after activation of these receptors, with IC50s ranging from 0.2 to 1.7 nM[2].

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

Cell Proliferation Assay[2]

Cell Line: Jeko-1, Mino, JVM2, Rec-1, Pfeiffer, SU-DHL-5, SU-DHL-6, WSU-NHL, SU-DHL-4, SU-DHL-8, and WILL-2 cells
Concentration: 0.1-3000 nM
Incubation Time: 4 days
Result: Resulted in a maximal inhibition of 70-90%, with IC50s of ≤10 nM in the four MCL cell lines.
Pfeiffer, SU-DHL-5, SU-DHL-6, and WSU-NHL were highly sensitive, with IC50s from 2 to 8 nM.
In Vivo

Parsaclisib (10 mg/kg; oral gavage twice daily for 7-19 days) inhibits tumor growth in the BALB/c mice bearing the A20 murine lymphoma cells[2].
Parsaclisib (0.1-10 mg/kg; p.o. twice daily) slows Pfeiffer xenograft tumor growth in a dose-dependent manner. And Parsaclisib was well tolerated[2].
Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473) in Pfeiffer subcutaneous mouse xenograft models[2].

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

Animal Model: Female BALB/c mice (5-9 weeks) were inoculated with A20 cells[2]
Dosage: 10 mg/kg
Administration: Oral gavage twice daily for 7-19 days
Result: Resulted in significant tumor growth inhibition (TGI).
Reduced the percentage of Tregs (CD4+CD25+FOXP3+) in tumors and spleens.
Increased the ratio of CD4+ and CD8+ T cells to Tregs in spleens and tumors.
Decreased the number of CD4+CD44high and CD8+CD44high T cells in both spleens and tumors.
Molecular Weight

469.34

Formula

C₂₀H₂₃Cl₂FN₆O₂

CAS No.

1995889-48-9

SMILES

CCOC1=C([[email protected]@H](C2)CNC2=O)C(F)=C(Cl)C=C1[[email protected]@H](N3C4=NC=NC(N)=C4C(C)=N3)C.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 240 mg/mL (511.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1307 mL 10.6533 mL 21.3065 mL
5 mM 0.4261 mL 2.1307 mL 4.2613 mL
10 mM 0.2131 mL 1.0653 mL 2.1307 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6 mg/mL (12.78 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ParsaclisibINCB050465INCB 050465INCB-050465PI3KPhosphoinositide 3-kinasePI3KδrelapsedrefractoryB-cellmalignanciesInhibitorinhibitorinhibit

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Parsaclisib hydrochloride
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