Parsaclisib (Synonyms: INCB050465; IBI-376)

Name: Parsaclisib
Brand: MedChemExpress
SKU: HY-109068
Rating: 4.5 (1 reviews)

Cat. No.: HY-109068 Purity: 99.31%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1426698-88-5

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 429	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 429	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 630	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3100	In-stock	Estimated Time of Arrival: December 31
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 hydrochloride In-stock

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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

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

432.88

Formula

C₂₀H₂₂ClFN₆O₂

CAS No.

1426698-88-5

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

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 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
Protocol 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
Protocol 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

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.
Protocol 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

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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.31%

Select Batch:

Data Sheet (279 KB) SDS (0 KB)

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

Handling Instructions (2659 KB)

References

[1]. Niu Shin, 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]

Complete Stock Solution Preparation Table

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

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:

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

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Parsaclisib (Synonyms: INCB050465; IBI-376)

Customer Review

Other Forms of Parsaclisib:

Parsaclisib Related Antibodies

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•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Parsaclisib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Parsaclisib Related Classifications

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