2. PI3K/Akt/mTOR
  3. PI3K
  4. Parsaclisib

Parsaclisib  (Synonyms: INCB050465; IBI-376)

Cat. No.: HY-109068 Purity: 99.31%
COA Handling Instructions

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

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

Parsaclisib Chemical Structure

Parsaclisib Chemical Structure

CAS No. : 1426698-88-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 429 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 429 In-stock
Solid
1 mg USD 185 In-stock
5 mg USD 390 In-stock
10 mg USD 630 In-stock
25 mg USD 1200 In-stock
50 mg USD 1950 In-stock
100 mg USD 3100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Parsaclisib:

Parsaclisib Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib 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.

Parsaclisib Related Antibodies

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.
Clinical Trial
Molecular Weight

432.88

Appearance

Solid

Formula

C20H22ClFN6O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (288.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3101 mL 11.5505 mL 23.1011 mL
5 mM 0.4620 mL 2.3101 mL 4.6202 mL
10 mM 0.2310 mL 1.1551 mL 2.3101 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

  • 5.

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

    Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.31%

COA (249 KB) HNMR (205 KB) RP-HPLC (237 KB) LCMS (89 KB)

Handling Instructions (2659 KB)
References
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Parsaclisib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

Parsaclisib1426698-88-5INCB050465 IBI-376INCB 050465INCB-050465IBI376IBI 376IBI-376PI3KPhosphoinositide 3-kinasePI3KδrelapsedrefractoryB-cellmalignanciesInhibitorinhibitorinhibit

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