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> Duvelisib [1201438-56-3]

Duvelisib [1201438-56-3]

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Référence HY-17044-10mg

Conditionnement : 10mg

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Duvelisib (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.

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Duvelisib Chemical Structure

Duvelisib Chemical Structure

CAS No. : 1201438-56-3

This product is a controlled substance and not for sale in your territory.

Based on 7 publication(s) in Google Scholar

Other Forms of Duvelisib:

  • Duvelisib (R enantiomer) In-stock

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Description

Duvelisib (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively[1][2].

IC50 & Target[2]

p110δ

2.5 nM (IC50)

p110γ

27.4 nM (IC50)

p110β

85 nM (IC50)

p110α

1602 nM (IC50)

In Vitro

PI3Kδ and PI3Kγ inhibition with Duvelisib (IPI-145) has anti-proliferative activity in primary AML cells by inhibiting the activity of AKT and MAPK. Pre-treatment of AML cells with Duvelisib inhibits both adhesion and migration of AML blasts to bone marrow stromal cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Duvelisib Related Antibodies
Essai clinique
Masse moléculaire

416.86

Formule

C22H17ClN6O
CAS No.

1201438-56-3
Appearance

Solid

Color

Off-white to gray

SMILES

O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)C)=CC5=C1C(Cl)=CC=C5
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : ≥ 41 mg/mL (98.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3989 mL 11.9944 mL 23.9889 mL
5 mM 0.4798 mL 2.3989 mL 4.7978 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

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

    Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
Pureté et documentation

Purity: 99.88%

COA (252 KB) RP-HPLC (208 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Pillinger G, et al. Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection. Oncotarget. 2016 Jun 28;7(26):39784-39795.  [Content Brief]

    [2]. G?ckeritz E, et al. Efficacy of phosphatidylinositol-3 kinase inhibitors with diverse isoform selectivity profiles for inhibiting the survival of chronic lymphocytic leukemia cells. Int J Cancer. 2015 Nov 1;137(9):2234-42.  [Content Brief]

  • [1]. Pillinger G, et al. Targeting PI3Kδ and PI3Kγ signalling disrupts human AML survival and bone marrow stromal cell mediated protection. Oncotarget. 2016 Jun 28;7(26):39784-39795.

    [2]. G?ckeritz E, et al. Efficacy of phosphatidylinositol-3 kinase inhibitors with diverse isoform selectivity profiles for inhibiting the survival of chronic lymphocytic leukemia cells. Int J Cancer. 2015 Nov 1;137(9):2234-42.

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3989 mL 11.9944 mL 23.9889 mL 59.9722 mL
5 mM 0.4798 mL 2.3989 mL 4.7978 mL 11.9944 mL
10 mM 0.2399 mL 1.1994 mL 2.3989 mL 5.9972 mL
15 mM 0.1599 mL 0.7996 mL 1.5993 mL 3.9981 mL
20 mM 0.1199 mL 0.5997 mL 1.1994 mL 2.9986 mL
25 mM 0.0960 mL 0.4798 mL 0.9596 mL 2.3989 mL
30 mM 0.0800 mL 0.3998 mL 0.7996 mL 1.9991 mL
40 mM 0.0600 mL 0.2999 mL 0.5997 mL 1.4993 mL
50 mM 0.0480 mL 0.2399 mL 0.4798 mL 1.1994 mL
60 mM 0.0400 mL 0.1999 mL 0.3998 mL 0.9995 mL
80 mM 0.0300 mL 0.1499 mL 0.2999 mL 0.7497 mL
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Duvelisib Related Classifications

Help & FAQs

Keywords:

Duvelisib1201438-56-3IPI-145 INK1197IPI145IPI 145INK1197INK 1197INK-1197PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Référence
Description
Cond.
Prix HT
HY-17044A-50mg
Duvelisib (R enantiomer) [1261590-48-0]
 50mg