| Field | Specification |
|---|---|
| Target | |
| Alternative names | INCB050465 hydrochloride; IBI-376 hydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H23Cl2FN6O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Parsaclisib hydrochloride, also known as INCB050465 hydrochloride or IBI-376 hydrochloride, is a potent, selective, orally active PI3Kδ inhibitor with an IC50 of 1 nM at 1 mM ATP. It shows approximately 20000-fold selectivity over other class I PI3K isoforms and can be used for research on relapsed or refractory B-cell malignancies[1][2][3]. It is supplied as a white to off-white solid (C20H23Cl2FN6O2, MW 469.34) at 99.33% purity.
Physical & Chemical Properties
| CAS Number | 1995889-48-9 |
|---|---|
| Molecular Formula | C20H23Cl2FN6O2 |
| Molecular Weight | 469.34 g/mol |
| Purity | 99.33% |
| 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 |
| Target | PI3Kδ |
| Signaling Pathway | PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: 100 mg/mL (213.07 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, stored under nitrogen, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PI3Kδ 1 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under 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).
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (213.07 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); stored under nitrogen, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 5 mg/mL (10.65 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 5 mg/mL (10.65 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (10.65 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | PBS |
|---|---|
| Result | 50 mg/mL (106.53 mM); clear solution; requires sonication |
Data provided by the manufacturer.
In Vitro
Proliferation of MCL and DLBCL cell lines is inhibited by Parsaclisib (0.1-3000 nM; 4 d)[2]. In the Ramos Burkitt’s lymphoma cell line, Parsaclisib (0.1-1000 nM; 2 h) inhibits anti-IgM-induced pAKT (Ser473), with an IC50 of 1 nM[2]. After activation of these receptors, Parsaclisib inhibits proliferation of human, dog, rat, and mouse primary B cells, with IC50s ranging from 0.2 to 1.7 nM[2].
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
In BALB/c mice bearing A20 murine lymphoma cells, Parsaclisib (oral gavage twice daily for 7-19 days; 10 mg/kg) suppresses tumor growth[2]. Parsaclisib (0.1-10 mg/kg; p.o. twice daily) slows Pfeiffer xenograft tumor growth dose-dependently, and Parsaclisib was well tolerated[2]. In Pfeiffer subcutaneous mouse xenograft models, Parsaclisib (0.5-1 mg/kg; a single p.o.) inhibits pAKT (Ser473)[2].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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A class I PI3K signalling network regulates primary cilia disassembly in normal physiology and disease. Nat Commun 2024 Aug 21;15(1):7181. PMID: 39168978
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. Cell Rep Methods 2026 Jun 15;6(6):101339. PMID: 42134319
A long-lasting PI3Kδ inhibitor zandelisib forms a water-shielded hydrogen bond with p110δ and demonstrates sustained inhibitory effects. Am J Cancer Res 2025 May 15;15(5):2097-2110. PMID: 40520883
