Duvelisib (Synonyms: IPI-145; INK1197)

目錄號(hào): HY-17044 純度: 99.88%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

Duvelisib (IPI-145) 是一種選擇性 p100δ 抑制劑，作用于 p110δ, p110γ, p110β 和 p110α，IC₅₀ 分別為 2.5 nM，27.4 nM，85 nM 和 1602 nM。

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Duvelisib Chemical Structure

CAS No. : 1201438-56-3

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可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥844	In-stock
1 mg	￥500	In-stock
5 mg	￥920	In-stock
10 mg	￥1300	In-stock
25 mg	￥2200	In-stock
50 mg	￥3300	In-stock
100 mg	￥4800	In-stock
200 mg		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

* Please select Quantity before adding items.

Customer Review

Other Forms of Duvelisib:

Duvelisib (R enantiomer) In-stock

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)

•Nat Metab. 2020 Dec;2(12):1427-1442. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]
•Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
•OncoImmunology. 11 Oct 2022.
•Arab J Chem. 2023 Jul 4, 105117.
•bioRxiv. 2024 October 02.
•Res Sq. 2024 Jun 13.
•bioRxiv. 2023 May 16.

Duvelisib 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 PI3K 亞型特異性產(chǎn)品:

查看所有亞型

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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)

細(xì)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]

體外研究
(In Vitro)

Duvelisib (IPI-145) 通過抑制 PI3Kδ 和 PI3Kγ 的活性，在急性髓系白血病 (AML) 原代細(xì)胞中表現(xiàn)抗增殖作用；預(yù)處理 AML 細(xì)胞可抑制其向骨髓基質(zhì)細(xì)胞的黏附和遷移^[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 號(hào)

1201438-56-3

性狀

固體

顏色

Off-white to gray

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 41 mg/mL (98.35 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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
10 mM	0.2399 mL	1.1994 mL	2.3989 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.88%

選擇批次：

Data Sheet (631 KB) SDS (393 KB)

COA (196 KB) RP-HPLC (208 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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]

Duvelisib 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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.

Keywords:

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

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MedChemExpress (MCE) 只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的用途提供醫(yī)藥研發(fā)服務(wù)，不為任何個(gè)人或者非科研性質(zhì)的、非用于藥證申報(bào)使用等其他用途提供服務(wù)。

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滬公網(wǎng)安備31011502019417

滬(浦)應(yīng)急管危經(jīng)許[2021]201709(QFYS)

營(yíng)業(yè)執(zhí)照（三證合一）

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Duvelisib (Synonyms: IPI-145; INK1197)

Customer Review

Other Forms of Duvelisib:

MCE 顧客使用本產(chǎn)品發(fā)表的 9 篇科研文獻(xiàn)