Parsaclisib hydrochloride (Synonyms: INCB050465 hydrochloride; IBI-376 hydrochloride)

Cat. No.: HY-109068A: Data Sheet
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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

CAS No. : 1995889-48-9

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Other In-stock Forms of Parsaclisib hydrochloride:

Parsaclisib

Other Forms of Parsaclisib hydrochloride:

Parsaclisib In-stock

1 Publications Citing Use of MCE Parsaclisib hydrochloride

•Nat Commun. 2024 Aug 21;15(1):7181. [Abstract]

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (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].

MedChemExpress (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⁺CD44^high and CD8⁺CD44^high T cells in both spleens and tumors.

Clinical Trial

Molecular Weight

469.34

Formula

C₂₀H₂₃Cl₂FN₆O₂

CAS No.

1995889-48-9

Appearance

Solid

Color

White to off-white

SMILES

CCOC1=C([C@@H](C2)CNC2=O)C(F)=C(Cl)C=C1[C@@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)

Purity & Documentation

Data Sheet (277 KB) SDS (252 KB) Handling Instructions (2659 KB)

References

[1]. Shin N, et al. Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. Cancer Research. 2015, Aug. 75(15).

[2]. Shin N, et, al. Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222. [Content Brief]

[3]. Yue EW, et, al. INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ). ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560. [Content Brief]

Parsaclisib hydrochloride Related Classifications

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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.

Keywords:

Parsaclisib1995889-48-9INCB050465IBI-376INCB 050465INCB-050465IBI376IBI 376PI3KPhosphoinositide 3-kinasePI3KδrelapsedrefractoryB-cellmalignanciesInhibitorinhibitorinhibit

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