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Tyrphostin AG 879

HER2 抑制剂，AG879是酪氨酸激酶的抑制剂，能够抑制TrKA的磷酸化，但不能抑制TrKB 和TrKC，也是高选择性的ErbB2激酶抑制剂。

目录号: PC16092 纯度: ≥98%

CAS No. :148741-30-4

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中文名称

Tyrphostin AG 879

英文名称

Tyrphostin AG 879

英文别名

2-Propenethioamide,3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)-;Tyrphostin AG 879;(E)-3-amino-2-[(3,5-ditert-butyl-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-3-sulfanylprop-2-enenitrile;AG 879;AG 879 (Tyrphostin AG 879);AG-879;2-Propenethioamide,3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-,(2E);BMK1-D4;Lopac-T-2067;α-Cyano-(3,5-di-t-butyl-4-hydroxy)thiocinnamide;(E)-3-[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-2-propenethioamide;TYRPHOSTIN 879;ALPHA-CYANO-(3,5-DI-T-BUTYL-4-HYDROXY)THIOCINNAMIDE;(3,5-DI-T-BUTYL-4-HYDROXYBENZYLIDENE)THIOCYANOACETAMIDE;ALPHA-CYANO-(3,5-DI-TERT-BUTYL-4-HYDROXY)THIOCINNAMAMIDE;2-CYANO-3-(3,5-DI-TERT-BUTYL-4-HYDROXYPHENYL)PROP-2-ENETHIOAMIDE;(E)-2-Cyano-3-(3,5-di-tert-butyl-4-hydroxyphenyl)prop-2-enethioamide;AG879;C18H24N2OS;(2E)-2-cyano-3-(3,5-di-tert-butyl-4-hydroxyphenyl)prop-2-enethioamide;tyrphostin AG879;BiomolKI_000028;BiomolKI2_000036;Lopac0_001175;BSPBio_001398;tyrphosti

Cas No.

148741-30-4

分子式

C₁₈H₂₄N₂Os

分子量

316.46

包装储存

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

生物活性

Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC₅₀ of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC₅₀ of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.

性状

Solid

IC50 & Target[1][2]

IC50: 10 μM (TrKA phosphorylation)
IC50: 1 μM (ErbB2)

体外研究(In Vitro)

Tyrphostin AG 879 (0.5-50 μM; 48 hours; HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells) treatment significantly and dose dependently decreases cell proliferation in all the cell lines.
Tyrphostin AG 879 (0.5-50 μM; 48 hours; HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells) treatment also induces a dose-dependent increase in apoptosis with the exception of the lines TE-671 and HTB-88 cells.

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

Cell Proliferation Assay

Cell Line:	HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells
Concentration:	0.5 μM, 5 μM, 20 μM and 50 μM
Incubation Time:	48 hours
Result:	Significantly and dose dependently decreased cell proliferation in all the cell lines.

Apoptosis Analysis

Cell Line:	HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells
Concentration:	0.5 μM, 5 μM, 20 μM and 50 μM
Incubation Time:	48 hours
Result:	Induced a dose-dependent increase in apoptosis.

体内研究(In Vivo)

Tyrphostin AG 879 (100 mg/kg;subcutaneous injection; administered 10 times in 19 days; for 21 days; athymic, immunodepressed NOD/SCID female mice) treatment induces in vivo a decrease in cancer growth in grafted athymic NOD/SCID mice.

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

Animal Model:	Athymic, immunodepressed NOD/SCID female mice (20 g) with HTB-114 and HL-60 cells
Dosage:	100 mg/kg
Administration:	Subcutaneous injection; administered 10 times in 19 days; for 21 days
Result:	Resulted in dramatic reductions in tumor sizes.

运输条件

Room temperature or refrigerated transportation.

储存方式

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

参考文献

[1]. Rende M et al. Role of nerve growth factor and its receptors in non-nervous cancer growth: efficacy of a tyrosine kinase inhibitor (AG879) and neutralizing antibodies antityrosine kinase receptor A and antinerve growth factor: an in-vitro and in-vivo stud [Information]

[2]. Zhou Y et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006 Jan 1;66(1):404-11.

[3]. Levitzki A, et al. Tyrosine kinase inhibition: an approach to drug development. Science. 1995 Mar 24;267(5205):1782-8. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (158.00 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1600 mL	15.7998 mL	31.5996 mL
5 mM	0.6320 mL	3.1600 mL	6.3199 mL
10 mM	0.3160 mL	1.5800 mL	3.1600 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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