NVP-TAE 226 (Synonyms: TAE226)

目录号: HY-13203 纯度: 99.77%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

NVP-TAE 226 (TAE226) 是一种有效且具有 ATP 竞争性的双重 FAK 和 IGF-1R 抑制剂，IC₅₀ 分别为 5.5 nM、140 nM。NVP-TAE 226 (TAE226) 还有效抑制 Pyk2，胰岛素受体 (InsR)，IC₅₀ 分为 3.5 nM、40 nM。

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NVP-TAE 226 Chemical Structure

CAS No. : 761437-28-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1377	In-stock
1 mg	￥554	In-stock
5 mg	￥1234	In-stock
10 mg	￥1989	In-stock
25 mg	￥3801	In-stock
50 mg	现货	询价
100 mg	现货	询价
200 mg		询价
500 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 10 篇科研文献

: NVP-TAE 226 purchased from MCE. Usage Cited in: Patent. US20170285005A1.; TAE226 reduces FAK activation and stretch-induced MMP-10 and MMP-12 expression in cultured podocytes.

: NVP-TAE 226 purchased from MCE. Usage Cited in: Patent. US20150175695A1.; The small molecule inhibitor for FAK, TAE226, reduces FAK activation and stretch-induced MMP-10 and MMP-12 expression in cultured podocytes. A) Podocytes are cultured on placental laminin in the presence or absence of TAE226 overnight. Extracts are prepared and analyzed by western blot for expression of pFAK397 and total FAK. FAK activation is also analyzed by western blot of podocyte extracts from stretched and non-stretched cells, demonstrating that biomechanical stretching directly activates

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC₅₀s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC₅₀s of 3.5 nM and 44 nM, respectively^[1]^[2].

IC₅₀ & Target

IC50: 5.5 nM (FAK), 3.5 nM (Pyk2), 140 nM (IGF-IR), 40 nM (InsR), 0.16 μM (c-Met), 0.36 μM (KDR), 0.48 μM (Flt3)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A 172	IC₅₀	8.3 μM Compound: TAE-226	Cytotoxicity against human A172 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A172 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33119295]
A375P	GI₅₀	1.69 μM Compound: TAE226	Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
A498	IC₅₀	0.81 μM Compound: TAE226	Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 34111829]
A549	IC₅₀	1.02 μM Compound: 1; TAE-226	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31550660]
A549	IC₅₀	1.16 μM Compound: TAE-226	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 31923858]
A549	IC₅₀	1.31 μM Compound: 1; TAE-226	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35486993]
ASPC1	IC₅₀	4.82 μM Compound: 1; TAE226	Antiproliferative activity against human ASPC1 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
ASPC1	IC₅₀	6.73 μM Compound: 1; TAE226	Antiproliferative activity against human AsPC1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human AsPC1 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
ASPC1	IC₅₀	6.73 μM Compound: 1; TAE226	Antiproliferative activity against human AsPC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human AsPC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
ASPC1	IC₅₀	6.73 μM Compound: TAE226	Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay	[PMID: 29102081]
BXPC-3	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
BXPC-3	IC₅₀	1.03 μM Compound: 1; TAE226	Antiproliferative activity against human BxPC3 cells after 72 hrs by CCK8 assay Antiproliferative activity against human BxPC3 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
BXPC-3	IC₅₀	1.03 μM Compound: TAE226	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 29102081]
CAKI-1	IC₅₀	1.05 μM Compound: TAE226	Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 34111829]
HCT-116	IC₅₀	0.23 μM Compound: TAE226	Inhibition of colony formation in human HCT116 cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human HCT116 cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
HCT-116	GI₅₀	0.27 μM Compound: TAE226	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
HCT-116	IC₅₀	0.29 μM Compound: 2; TAE226	Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
HCT-116	IC₅₀	0.39 μM Compound: TAE-226	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability by WST1 assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability by WST1 assay	[PMID: 28284808]
HCT-116	IC₅₀	0.4 μM Compound: TAE226	Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay Antiproliferative activity against human HCT116 cells after 48 hrs by WST-1 assay	[PMID: 25180654]
HK-2	IC₅₀	8.2 μM Compound: TAE-226	Cytotoxicity against human HK2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human HK2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 31923858]
HK-2	IC₅₀	8.2 μM Compound: 1; TAE-226	Cytotoxicity against human HK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31550660]
HUVEC	IC₅₀	1 μM Compound: TAE-226	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-stimulated proliferation after 72 hrs by WST-1 assay	[PMID: 23845217]
KM3/BTZ	IC₅₀	4.386 μM Compound: 1; TAE226	Antiproliferative activity against bortezomib- resistant human KM3/BTZ cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against bortezomib- resistant human KM3/BTZ cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
L02	IC₅₀	5.212 μM Compound: 1; TAE226	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
L02	IC₅₀	5.37 μM Compound: 1; TAE226	Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
L02	IC₅₀	5.37 μM Compound: 1; TAE226	Cytotoxicity against human L02 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
MCF-10A	IC₅₀	8.76 μM Compound: 2; TAE226	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
MCF7	IC₅₀	0.45 μM Compound: 2; TAE226	Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
MDA-MB-231	GI₅₀	1.49 μM Compound: TAE226	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
MDA-MB-231	IC₅₀	1.9 μM Compound: TAE226	Inhibition of colony formation in human MDA-MB-231 cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human MDA-MB-231 cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
MDA-MB-231	IC₅₀	2.8 μM Compound: TAE226	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST-1 assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST-1 assay	[PMID: 25180654]
MDA-MB-231	IC₅₀	4.06 μM Compound: TAE-226	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 31923858]
MDA-MB-231	IC₅₀	4.24 μM Compound: 1; TAE-226	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31550660]
MIA PaCa-2	IC₅₀	5.23 μM Compound: 1; TAE226	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS,TP53,CDKN2A and DPC4/SMAD4 mutations assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
NCI/ADR-RES	IC₅₀	> 5 μM Compound: 1; TAE226	Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
NCI-H1975	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
NCI-H1975	IC₅₀	> 2 μM Compound: 1; TAE226	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
PANC-1	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against human PANC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30978560]
PANC-1	IC₅₀	> 20 μM Compound: 1; TAE226	Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay	[PMID: 28576633]
PANC-1	IC₅₀	> 20 μM Compound: TAE226	Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay Antiproliferative activity against human PANC1 cells after 72 hrs by MTT assay	[PMID: 29102081]
PC-3	IC₅₀	0.26 μM Compound: TAE226	Inhibition of colony formation in human PC3 cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human PC3 cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
PC-3	IC₅₀	1.21 μM Compound: 2; TAE226	Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
PC-3	IC₅₀	1.6 μM Compound: TAE226	Antiproliferative activity against human PC3 cells after 48 hrs by WST-1 assay Antiproliferative activity against human PC3 cells after 48 hrs by WST-1 assay	[PMID: 25180654]
Raji	IC₅₀	> 10 μM Compound: 1; TAE226	Antiproliferative activity against human Raji cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35872546]
Sf9	IC₅₀	6.79 nM Compound: 1; TAE226	Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo assay Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo assay	[PMID: 30978560]
U-251	IC₅₀	6.3 μM Compound: TAE-226	Cytotoxicity against human U251 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human U251 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33119295]
U-87MG ATCC	IC₅₀	0.19 μM Compound: TAE226	Inhibition of colony formation in human U87MG cells after 2 weeks by crystal violet staining-based assay Inhibition of colony formation in human U87MG cells after 2 weeks by crystal violet staining-based assay	[PMID: 25180654]
U-87MG ATCC	IC₅₀	1.2 μM Compound: TAE226	Antiproliferative activity against human U87MG cells after 48 hrs by WST-1 assay Antiproliferative activity against human U87MG cells after 48 hrs by WST-1 assay	[PMID: 25180654]
U-87MG ATCC	IC₅₀	1.3 μM Compound: TAE-226	Cytotoxicity against human U87MG cells assessed as reduction in cell viability by WST1 assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability by WST1 assay	[PMID: 28284808]
U-87MG ATCC	IC₅₀	1.58 μM Compound: 2; TAE226	Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
U-87MG ATCC	IC₅₀	1.67 μM Compound: TAE-226	Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human U-87MG cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 31923858]
U-87MG ATCC	IC₅₀	2.9 μM Compound: TAE-226	Cytotoxicity against human U-87 MG cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human U-87 MG cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33119295]
U-87MG ATCC	EC₅₀	41 nM Compound: 41	Inhibition of JNK in human U87MG cells overexpressing EGFR V3 mutant assessed as inhibition of c-jun phosphorylation after 6 hrs by ELISA Inhibition of JNK in human U87MG cells overexpressing EGFR V3 mutant assessed as inhibition of c-jun phosphorylation after 6 hrs by ELISA	10.1039/C1MD00219H

体外研究
(In Vitro)

NVP-TAE 226 (TAE226)，一种有效的 ATP 竞争性抑制剂，可抑制多种酪氨酸蛋白激酶，尤其是 FAK 和 IGF-IR 激酶。在基于细胞的激酶测定中，FAK、IGF-IR 激酶和 IR 激酶受到抑制，IC₅₀ 范围为 100 至 300 nM，与其他测试的激酶相比不太敏感，IC₅₀ 均高出 10 倍。在培养物中，NVP-TAE 226 抑制细胞外基质诱导的 FAK (Tyr³⁹⁵) 自磷酸化。NVP-TAE 226 还抑制 IGF-I 诱导的 IGF-IR 磷酸化及其下游靶基因 (如 MAPK 和 Akt) 的活性。NVP-TAE 226 可延缓肿瘤细胞生长 (通过细胞活力测定评估) 并减弱与细胞周期蛋白 B1 和磷酸化 cdc2 (Tyr¹⁵) 减少相关的 G₂-M 细胞周期进程>) 蛋白表达。在体外 Matrigel 侵袭试验中，与对照相比，NVP-TAE 226 处理抑制肿瘤细胞侵袭至少 50%。有趣的是，TAE226 处理含有野生型 p53 的肿瘤细胞主要表现为 G₂-M 阻滞，而含有突变型 p53 的肿瘤细胞发生凋亡^[1]。

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

体内研究
(In Vivo)

用 50 或 75 mg/kg 的 NVP-TAE 226 (TAE226) 处理分别将 U87 肿瘤异种移植动物的中位存活期延长 6 天和 7 天 (与对照组处理的动物相比，分别为 P=0.084 和 P=0.042)。然而，NVP-TAE 226 处理 LN229 肿瘤异种移植的动物可显著延长其中位生存期 19 天 (与载体处理的动物相比，两种剂量的 P<0.004)^[1]。

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

分子量

468.94

Formula

C₂₃H₂₅ClN₆O₃

CAS 号

761437-28-9

性状

固体

颜色

Light yellow to yellow

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 11.11 mg/mL (23.69 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1325 mL	10.6623 mL	21.3247 mL
5 mM	0.4265 mL	2.1325 mL	4.2649 mL
10 mM	0.2132 mL	1.0662 mL	2.1325 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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: 1.11 mg/mL (2.37 mM); 悬浊液; 超声助溶

此方案可获得 1.11 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 11.1 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% Corn Oil
Solubility: 1.11 mg/mL (2.37 mM); 澄清溶液; 超声助溶

此方案可获得 1.11 mg/mL的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： 50% PEG300 50% Saline
Solubility: 3.33 mg/mL (7.10 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (10.66 mM); 悬浊液; 超声助溶

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

每只动物的给药体积

μL

动物数量

只

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: 99.77%

选择批次：

Data Sheet (651 KB) SDS (393 KB)

COA (192 KB) LCMS (123 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Liu TJ, et al. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther, 2007, 6(4), 1357-1367. [Content Brief]

[2]. Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9(6):e99083. [Content Brief]

[3]. Lietha D, et al. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One. 2008;3(11):e3800. [Content Brief]

Cell Assay ^[1]	Glioma cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2×10⁴ in 24-well culture plates for 24 h before drug treatment. Culture medium is used for mock treatment. Cells are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyzer. The antiproliferative activity of NVP-TAE 226 (ranging from 0.25 to 1 μM) on cells growing in culture is determined using a tetrazolium-based colorimetric MTT assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Male nude mice used for this study are 6 to 8 weeks old. In DMEM/F12 serum-free media (5 μL), 5×10⁵ of U87 cells and 1×10⁶ of LN229 cells per mouse are implanted intracranially through a guide-screw system. Four days after injection of the tumor cells, mice are randomized into three groups for each cell line (n=6). Mice in group 1 are treated with 50 mg/kg NVP-TAE 226 in 200 μL of 0.5% methylcellulose, via an oral gavage. The mice in group 2 receive 75 mg/kg NVP-TAE 226 in 200 μL of 0.5% methylcellulose. The mice in group 3 the same vehicle used for administration of NVP-TAE 226 (control). Treatment frequency is once a day for 5 days and off for 2 days, for a duration of 4 weeks. Mice are monitored daily. Mice are euthanized when they are moribund, and the whole brain is extracted for rapid freezing in liquid nitrogen and storage at -70°C. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Liu TJ, et al. Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. Mol Cancer Ther, 2007, 6(4), 1357-1367. [Content Brief] [2]. Delimont D, et al. Laminin α2-mediated focal adhesion kinase activation triggers Alport glomerular pathogenesis. PLoS One. 2014 Jun 10;9(6):e99083. [Content Brief] [3]. Lietha D, et al. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One. 2008;3(11):e3800. [Content Brief]

NVP-TAE 226 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1325 mL	10.6623 mL	21.3247 mL	53.3117 mL
	5 mM	0.4265 mL	2.1325 mL	4.2649 mL	10.6623 mL
	10 mM	0.2132 mL	1.0662 mL	2.1325 mL	5.3312 mL
	15 mM	0.1422 mL	0.7108 mL	1.4216 mL	3.5541 mL
	20 mM	0.1066 mL	0.5331 mL	1.0662 mL	2.6656 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 226761437-28-9TAE226TAE 226TAE-226FAKPyk2IGF-1RInsulin ReceptorApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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NVP-TAE 226 (Synonyms: TAE226)

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MCE 顾客使用本产品发表的 10 篇科研文献

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NVP-TAE 226 (Synonyms: TAE226)

Customer Review

NVP-TAE 226 相关抗体

MCE 顾客使用本产品发表的 10 篇科研文献

NVP-TAE 226 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

NVP-TAE 226 相关抗体:

摩尔计算器

稀释计算器

NVP-TAE 226 相关分类

完整储备液配制表

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