NVP-TAE 684 (Synonyms: TAE 684)

目錄號: HY-10192 純度: 99.27%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術支持

NVP-TAE 684 (TAE 684) 是一種高效的，選擇性的 ALK 抑制劑，阻止 ALCL 衍生的 ALK 依賴性細胞株的生長，IC₅₀ 值為 2-10 nM。

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NVP-TAE 684 Chemical Structure

CAS No. : 761439-42-3

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規(guī)格	價格	是否有貨
1 mg	￥340	In-stock
5 mg	￥750	In-stock
10 mg	￥1150	In-stock
25 mg	￥2100	In-stock
50 mg	￥3150	In-stock
100 mg	￥4350	In-stock
200 mg		詢價
500 mg		詢價

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 14 篇科研文獻

•Theranostics. 2020 Apr 6;10(11):5120-5136. [Abstract]
•Cell Chem Biol. 2022 Aug 29;S2451-9456(22)00311-7. [Abstract]
•Cell Chem Biol. 2018 Feb 15;25(2):224-229.e2. [Abstract]
•Pigment Cell Melanoma Res. 2016 May;29(3):284-96. [Abstract]
•Biomolecules. 2024 May 28.
•Mol Cancer Res. 2022 Mar.

•Pigment Cell Melanoma Res. 2019 May;32(3):391-402. [Abstract]
•BMC Biol. 2018 Sep 5;16(1):90. [Abstract]
•Pigment Cell Melanoma Res. 2016 May;29(3):284-96. [Abstract]
•J Gene Med. 2022 Sep 30;e3451. [Abstract]
•Cancer Chemother Pharmacol. 2018 Aug;82(2):251-263. [Abstract]
•ACS Chem Biol. 2012 Dec 21;7(12):1968-74. [Abstract]
•Department Biologie. Eberhard Karls Universität Tübingen. 2016 Jan.
•Harvard Medical School LINCS LIBRARY

: NVP-TAE 684 purchased from MCE. Usage Cited in: Pigment Cell Melanoma Res. 2016 May;29(3):284-96. [Abstract]; Ltk inhibitor TAE684 partially rescues the ltk^mne phenotype and decreases the number of iridophores. The number of iridophores is reduced in ltk^mne/+ larvae treated with ALK inhibitor TAE684 from 82 to 105 hpf.

: NVP-TAE 684 purchased from MCE. Usage Cited in: ACS Chem Biol. 2012 Dec 21;7(12):1968-74. [Abstract]; TAE684 inhibits NPM-Ltk. Wild-type embryos are injected with 30 pg of psox10:NPM-Ltk and treated with 3 μM of TAE684. Incident light images at 3 dpf of control uninjected, nontreated embryo (a); NPM-Ltk injected, DMSO-treated sibling (b); and NPM-Ltk injected TAE684-treated siblings (c).

NVP-TAE 684 相關產(chǎn)品

•相關化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

生物活性
實驗參考方法
純度 & 產(chǎn)品資料
參考文獻

生物活性

NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC₅₀ values between 2 and 10 nM^[1].

IC₅₀ & Target

IC50: 2-10 nM (ALK-dependent cell lines)^[1]

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.001 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay	[PMID: 21572589]
BaF3	IC₅₀	0.02 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay	[PMID: 21572589]
BaF3	IC₅₀	0.06 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay Cytotoxicity against mouse BAF3 cells expressing ALK F1174L mutant coexpressing EML4 after 48 hrs by MTS assay	[PMID: 21572589]
BaF3	IC₅₀	0.08 μM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay	[PMID: 21572589]
BaF3	GI₅₀	1.1 μM Compound: 14; TAE684	Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
BaF3	IC₅₀	1336 nM Compound: 4, TAE684	Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	IC₅₀	229.3 nM Compound: 18; TAE684	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	3 nM Compound: 1, TAE684	Cytotoxicity against mouse BAF3 cells expressing NPM-ALK after 48 hrs by CellTiter-Glo assay Cytotoxicity against mouse BAF3 cells expressing NPM-ALK after 48 hrs by CellTiter-Glo assay	[PMID: 21572589]
BaF3	IC₅₀	3.7 nM Compound: 4, TAE684	Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
BaF3	IC₅₀	340.7 nM Compound: 18; TAE684	Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing human EGFR C797S/T790M/del19 mutant assessed as inhibition of in cell viability measured after 72 hrs by CellTiter-Glo assay	[PMID: 33243531]
BaF3	IC₅₀	43.7 nM Compound: 4, TAE684	Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
HEK293	IC₅₀	21.9 nM Compound: TAE684	Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	6.1 nM Compound: TAE684	Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	7.8 nM Compound: TAE684	Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	93.3 nM Compound: TAE684	Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
KARPAS-299	IC₅₀	< 10 nM Compound: TAE-684	Decrease in ALK phosphorylation in human Karpas299 cells after 4 hrs Decrease in ALK phosphorylation in human Karpas299 cells after 4 hrs	[PMID: 17185414]
KARPAS-299	IC₅₀	13 nM Compound: 2, NVP-TAE684	Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs	[PMID: 24900831]
KARPAS-299	IC₅₀	14 nM Compound: 7; TAE684	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
KARPAS-299	IC₅₀	2 nM Compound: TAE-684	Antiproliferative activity against human Karpas299 cells assessed as luciferase expression after 72 hrs Antiproliferative activity against human Karpas299 cells assessed as luciferase expression after 72 hrs	[PMID: 17185414]
KARPAS-299	IC₅₀	2.4 nM Compound: 4, TAE684	Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay	[PMID: 23742252]
KARPAS-299	IC₅₀	3 nM Compound: TAE-684	Induction of apoptosis in human Karpas299 cells by annexin V assay Induction of apoptosis in human Karpas299 cells by annexin V assay	[PMID: 17185414]
NCI-H1975	GI₅₀	0.72 μM Compound: 14; TAE684	Growth inhibition of human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28850922]
SU-DHL-1	IC₅₀	2 nM Compound: TAE-684	Antiproliferative activity against human SUDHL1 cells assessed as luciferase expression after 72 hrs Antiproliferative activity against human SUDHL1 cells assessed as luciferase expression after 72 hrs	[PMID: 17185414]

體外研究
(In Vitro)

TAE684 抑制 Ba/F3 NPM-ALK 細胞的增殖，IC₅₀ 為 3 nM，濃度高達 1 μM 時不影響親代 Ba/F3 細胞的存活。TAE684 在 Ba/F3 NPM-ALK 和 Karpas-299 細胞中以劑量依賴性方式抑制 STAT3 和 STAT5 磷酸化。TAE684 在表達 NPM-ALK 的 Ba/F3 細胞和 ALCL 細胞系中誘導細胞凋亡和 G1 期阻滯^[1]。
NVP-TAE684 顯著降低敏感 H3122 和 H3122 CR 細胞的細胞存活率，但對其他非 ALK 依賴性癌細胞系的活力幾乎沒有影響。NVP-TAE684處理H3122 CR細胞抑制ALK、AKT和ERK的磷酸化并誘導顯著的細胞凋亡。
TAE684有效抑制表達EML4-ALK L1196M突變體的Ba/F3細胞的存活^[2]。
mALKR1279Q 突變體表達誘導的神經(jīng)突生長在 30 nM NVP-TAE684 下被完全抑制，這與激活的 wt mALK所見的反應相當^[3]。

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

體內研究
(In Vivo)

NVP-TAE684 在兩個獨立的 ALK 陽性 ALCL 模型中抑制淋巴瘤形成，并誘導已建立的 Karpas-299 淋巴瘤消退。NVP-TAE684 在體內顯示出可觀的生物利用度和半衰期。
NVP-TAE684 (1、3 和 10 mg/kg. po) 顯著延遲淋巴瘤的發(fā)展，并顯示發(fā)光信號減少 100 到 1,000 倍。NVP-TAE684 (10 mg/kg) 處理組看起來很健康，沒有表現(xiàn)出任何化合物或疾病相關毒性的跡象^[1]。

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

分子量

614.20

Formula

C₃₀H₄₀ClN₇O₃S

CAS 號

761439-42-3

性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 7.69 mg/mL (12.52 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

1 mM	1.6281 mL	8.1407 mL	16.2813 mL
5 mM	0.3256 mL	1.6281 mL	3.2563 mL
10 mM	0.1628 mL	0.8141 mL	1.6281 mL

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

摩爾計算器
稀釋計算器

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)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.77 mg/mL (1.25 mM); 澄清溶液

此方案可獲得 ≥ 0.77 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 7.7 mg/mL 的澄清 DMSO 儲備液加到 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

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.77 mg/mL (1.25 mM); 澄清溶液

此方案可獲得 ≥ 0.77 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 7.7 mg/mL 的澄清 DMSO 儲備液加到 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。

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動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。，Tween 80，均可在 MCE 網(wǎng)站選購。

計算結果

工作液所需濃度 : mg/mL

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

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。

動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，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，請謹慎選擇該方案。

請確保第一步儲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: 99.27%

選擇批次：

Data Sheet (649 KB) SDS (393 KB)

COA (173 KB) HNMR (170 KB) RP-HPLC (60 KB) MS (66 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[1]. Galkin AV, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. [Content Brief]

[2]. Katayama R, et al. Therapeutic strategies to overcome PF-02341066 resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. [Content Brief]

[3]. Schonherr C, Activating ALK mutations found in neuroblastoma are inhibited by PF-02341066 and NVP-TAE684. Biochem J. 2011 Dec 15;440(3):405-13. [Content Brief]

Cell Assay ^[1]	Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, BCR-ABL, or TEL-kinase fusion constructs are plated in 384-well plates (25,000 cells per well) and incubated with serial dilutions of TAE684 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. ICsub>50?values are generated by using XLFit software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	For in vivo compound efficacy studies, treatment is initiated 72 h after tail vein injection of 1×10⁶ Karpas-299-, Ba/F3 NPM-ALK- or BCR-ABL-expressing cells into female Fox Chase SCIDBeige mice. Mice (n=10 per group) are administered either TAE684 resuspended in 10% 1-methyl-2-pyrrolidinone/90% PEG 300 solution at 1, 3, and 10 mg/kg once daily for 3 weeks or the vehicle solution at the same dosing schedule. Disease progression and compound efficacy is monitored weekly with bioluminescence imaging. To determine the efficacy of TAE684 on established disease, dosing is initiated on day 12, at which time the disease confirmed to be widespread by bioluminescence imaging. For analysis of downstream molecular effects in vivo, mice with established lymphomas are administered vehicle solution or TAE684 (10 mg/kg) for 3 days. At the end of treatment, mice are killed, and lymph nodes are extracted for immunoblotting and histological analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[1]. Galkin AV, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. [Content Brief] [2]. Katayama R, et al. Therapeutic strategies to overcome PF-02341066 resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. [Content Brief] [3]. Schonherr C, Activating ALK mutations found in neuroblastoma are inhibited by PF-02341066 and NVP-TAE684. Biochem J. 2011 Dec 15;440(3):405-13. [Content Brief]

NVP-TAE 684 相關分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6281 mL	8.1407 mL	16.2813 mL	40.7034 mL
	5 mM	0.3256 mL	1.6281 mL	3.2563 mL	8.1407 mL
	10 mM	0.1628 mL	0.8141 mL	1.6281 mL	4.0703 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:

NVP-TAE 684761439-42-3TAE 684TAE684TAE-684Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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NVP-TAE 684 (Synonyms: TAE 684)

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 14 篇科研文獻

NVP-TAE 684 相關產(chǎn)品

•相關化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

生物活性

實驗參考方法

純度 & 產(chǎn)品資料

參考文獻

摩爾計算器

稀釋計算器

NVP-TAE 684 相關分類

完整儲備液配制表

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NVP-TAE 684 (Synonyms: TAE 684)

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NVP-TAE 684 相關抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 14 篇科研文獻

NVP-TAE 684 相關產(chǎn)品

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生物活性

實驗參考方法

純度 & 產(chǎn)品資料

參考文獻

NVP-TAE 684 相關抗體:

摩爾計算器

稀釋計算器

NVP-TAE 684 相關分類

完整儲備液配制表

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