1. PI3K/Akt/mTOR
  2. PI3K
  3. Duvelisib

Duvelisib  (Synonyms: IPI-145; INK1197)

製品番号: HY-17044 純度: 99.88%
COA 取扱説明書 Technical Support

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 構造式

Duvelisib 構造式

CAS 番号 : 1201438-56-3

容量 価格(税別) 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 85 在庫あり
Solution
10 mM * 1 mL in DMSO USD 85 在庫あり
Solid
5 mg USD 77 在庫あり
10 mg USD 110 在庫あり
50 mg USD 209 在庫あり
100 mg USD 343 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Other Forms of Duvelisib:

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
4T1 IC50
22.88 μM
Compound: Duvelisib
Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against mouse 4T1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
A549 IC50
> 100 μM
Compound: Duvelisib
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
B16-F10 IC50
> 100 μM
Compound: Duvelisib
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
DOHH-2 IC50
0.2 μM
Compound: 1; IPI-145
Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
HepG2 IC50
> 100 μM
Compound: Duvelisib
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
Huh-7 IC50
6.57 μM
Compound: Duvelisib
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
Jurkat IC50
1.9 μM
Compound: Duvelisib
Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay
Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay
[PMID: 27774127]
Jurkat IC50
3.17 μM
Compound: Duvelisib
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
L929 IC50
> 100 μM
Compound: Duvelisib
Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
LOUCY IC50
0.98 μM
Compound: Duvelisib
Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay
Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay
[PMID: 27774127]
MCF7 IC50
> 100 μM
Compound: Duvelisib
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
MDA-MB-231 IC50
9.76 μM
Compound: Duvelisib
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
MOLM-14 IC50
1.2 μM
Compound: Duvelisib
Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay
Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay
[PMID: 27774127]
MOLT-4 IC50
2.3 μM
Compound: Duvelisib
Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay
Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay
[PMID: 27774127]
MV4-11 IC50
4.4 μM
Compound: Duvelisib
Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay
[PMID: 27774127]
Ramos IC50
0.001 μM
Compound: 4; IPI-145
Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins
Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins
[PMID: 31033293]
RAW264.7 IC50
0.025 μM
Compound: 4; IPI-145
Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins
Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins
[PMID: 31033293]
RAW264.7 IC50
13.2 μM
Compound: Duvelisib
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
Sf21 IC50
0.001 μM
Compound: 4; IPI-145
Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po
Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po
[PMID: 31033293]
Sf21 IC50
0.008 μM
Compound: 4; IPI-145
Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol
Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol
[PMID: 31033293]
SUD4 IC50
0.27 μM
Compound: 1; IPI-145
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
SU-DHL-6 IC50
0.39 μM
Compound: 1; IPI-145
Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
SU-DHL-6 IC50
0.4 nM
Compound: 1; IPI-145
Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human SUDHL2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35831917]
T47D IC50
> 100 μM
Compound: Duvelisib
Cytotoxicity against human T47D cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human T47D cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
THP-1 IC50
14.89 μM
Compound: Duvelisib
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 37011446]
体外実験

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.

臨床実験
分子量

416.86

分子式

C22H17ClN6O

CAS 番号
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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (239.89 mM; ultrasonic and warming and heat to 60°C; 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 2.3989 mL 11.9944 mL 23.9889 mL
5 mM 0.4798 mL 2.3989 mL 4.7978 mL
10 mM 0.2399 mL 1.1994 mL 2.3989 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

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体積 (開始)

V1

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体内:

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: ≥ 5 mg/mL (11.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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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.
純度とドキュメンテーション

純度: 99.88%

参考文献

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
100 mM 0.0240 mL 0.1199 mL 0.2399 mL 0.5997 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
Duvelisib
製品番号:
HY-17044
数量:
MCE 日本正規代理店: