Parsaclisib
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.71%
- No. CAS: 1426698-88-5
- Fòrmula: C20H22ClFN6O2
- Peso molecular:432.88
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Parsaclisib
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PI3Kδ 1 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
0.15 nM
Compound: 4; INCB-050465
|
Cytotoxicity against human B cells
Cytotoxicity against human B cells
|
[PMID: 30582813] |
| HEK293 | IC50 |
75 μM
Compound: 20; INCB050465
|
Inhibition of human ERG expressed in HEK293 cells by voltage patch clamp assay
Inhibition of human ERG expressed in HEK293 cells by voltage patch clamp assay
|
[PMID: 31749910] |
| Pfeiffer | IC50 |
2.5 nM
Compound: 20; INCB050465
|
Cytotoxicity against human Pfeiffer cells assessed as reduction in cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
Cytotoxicity against human Pfeiffer cells assessed as reduction in cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
|
[PMID: 31749910] |
| Pfeiffer | IC50 |
4.2 nM
Compound: 20; INCB050465
|
Cytotoxicity against human Pfeiffer cells assessed as reduction in protein binding adjusted cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
Cytotoxicity against human Pfeiffer cells assessed as reduction in protein binding adjusted cell viability incubated for 4 days by [3H]-thymidine incorporation based liquid scintillation counter method
|
[PMID: 31749910] |
| Ramos | IC50 |
1.1 nM
Compound: 20; INCB050465
|
Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in AKT phosphorylation incubated for 2 hrs by Alexa flour 488 based FACS analysis
Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in AKT phosphorylation incubated for 2 hrs by Alexa flour 488 based FACS analysis
|
[PMID: 31749910] |
| SU-DHL-6 | IC50 |
1.6 nM
Compound: 20; INCB050465
|
Cytotoxicity against human SUDHL6 cells assessed as reduction in cell viability incubated for 4 days by celltiter glo luminescent assay
Cytotoxicity against human SUDHL6 cells assessed as reduction in cell viability incubated for 4 days by celltiter glo luminescent assay
|
[PMID: 31749910] |
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 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 (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+CD44high and CD8+CD44high T cells in both spleens and tumors.
Chemical Information
-
No. CAS 1426698-88-5
-
Appearance Solid
-
Peso molecular 432.88
-
Fòrmula C20H22ClFN6O2
-
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
-
Synonyms
INCB050465; IBI-376
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
A class I PI3K signalling network regulates primary cilia disassembly in normal physiology and disease. [Abstract]2024 Aug 21;15(1):7181. PMID: 39168978 -
Cell Rep Methods
Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]2026 Jun 15;6(6):101339. PMID: 42134319 -
Am J Cancer Res
A long-lasting PI3Kδ inhibitor zandelisib forms a water-shielded hydrogen bond with p110δ and demonstrates sustained inhibitory effects. [Abstract]2025 May 15;15(5):2097-2110. PMID: 40520883
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (288.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3101 mL | 11.5505 mL | 23.1011 mL | 57.7527 mL |
| 5 mM | 0.4620 mL | 2.3101 mL | 4.6202 mL | 11.5505 mL | |
| 10 mM | 0.2310 mL | 1.1551 mL | 2.3101 mL | 5.7753 mL | |
| 15 mM | 0.1540 mL | 0.7700 mL | 1.5401 mL | 3.8502 mL | |
| 20 mM | 0.1155 mL | 0.5775 mL | 1.1551 mL | 2.8876 mL | |
| 25 mM | 0.0924 mL | 0.4620 mL | 0.9240 mL | 2.3101 mL | |
| 30 mM | 0.0770 mL | 0.3850 mL | 0.7700 mL | 1.9251 mL | |
| 40 mM | 0.0578 mL | 0.2888 mL | 0.5775 mL | 1.4438 mL | |
| 50 mM | 0.0462 mL | 0.2310 mL | 0.4620 mL | 1.1551 mL | |
| 60 mM | 0.0385 mL | 0.1925 mL | 0.3850 mL | 0.9625 mL | |
| 80 mM | 0.0289 mL | 0.1444 mL | 0.2888 mL | 0.7219 mL | |
| 100 mM | 0.0231 mL | 0.1155 mL | 0.2310 mL | 0.5775 mL |
Parsaclisib Related Classifications
HY-109068 Related Classifications
Powered by Bioz