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

Duvelisib  (Synonyms: IPI-145; INK1197)

目录号: HY-17044 纯度: 99.88%
COA 产品使用指南

Duvelisib (IPI-145) 是一种选择性 p100δ 抑制剂,作用于 p110δ, p110γ, p110β 和 p110α,IC50 分别为 2.5 nM,27.4 nM,85 nM 和 1602 nM。

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Duvelisib Chemical Structure

Duvelisib Chemical Structure

CAS No. : 1201438-56-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥844
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1 mg ¥500
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5 mg ¥920
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10 mg ¥1300
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25 mg ¥2200
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50 mg ¥3300
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100 mg ¥4800
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Customer Review

Other Forms of Duvelisib:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(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]
体外研究
(In Vitro)

Duvelisib (IPI-145) 通过抑制 PI3KδPI3Kγ 的活性,在急性髓系白血病 (AML) 原代细胞中表现抗增殖作用;预处理 AML 细胞可抑制其向骨髓基质细胞的黏附和迁移[1].

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

Clinical Trial
分子量

416.86

Formula

C22H17ClN6O

CAS 号
性状

固体

颜色

Off-white to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 41 mg/mL (98.35 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.88%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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产品名称:
Duvelisib
目录号:
HY-17044
需求量: