Tyrphostin AG 879(Synonyms: AG 879)

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Tyrphostin AG 879 (Synonyms: AG 879) 纯度: 99.54%

Tyrphostin AG 879 (AG 879) 是一种抑制 TrKA 磷酸化 (IC50 为 10 μM) 但不抑制 TrKB 和 TrKC 的酪氨酸激酶抑制剂。Tyrphostin AG 879 还是一种选择性的 ErbB2 酪氨酸激酶抑制剂，IC50 为 1 μM，对 ErbB2 的选择性至少比 EGFR 高 500 倍。Tyrphostin AG 879 具有抗癌活性。

Tyrphostin AG 879(Synonyms: AG 879)

Tyrphostin AG 879 Chemical Structure

CAS No. : 148741-30-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥800 In-stock
25 mg ￥1900 In-stock
50 mg ￥3200 In-stock
100 mg ￥5500 In-stock
200 mg   询价  
500 mg   询价  

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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[1][2][3].

IC50 & Target

IC50: 10 μM (TrKA phosphorylation)[1]
IC50: 1 μM (ErbB2)[2]
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[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[1]

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[1].

上海金畔生物科技有限公司 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[1]
Dosage: 100 mg/kg
Administration: Subcutaneous injection; administered 10 times in 19 days; for 21 days
Result: Resulted in dramatic reductions in tumor sizes.

分子量

316.46

Formula

C18H24N2OS
CAS 号

148741-30-4
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

配制储备液
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

*

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, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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 study. Anticancer Drugs. 2006 Sep;17(8):929-41.

    [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.

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