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Tyrphostin AG 879
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Tyrphostin AG 879图片
CAS NO:148741-30-4
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
AG 879
产品介绍
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。
生物活性

Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibitsTrKAphosphorylation (IC50of 10 μM), but notTrKBandTrKC. Tyrphostin AG 879 is also a selectiveErbB2tyrosine kinase inhibitor with anIC50of 1 μM, and has at least 500-fold higher selectivity toErbB2thanEGFR. 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].

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].

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

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.1600 mL15.7998 mL31.5996 mL
5 mM0.6320 mL3.1600 mL6.3199 mL
10 mM0.3160 mL1.5800 mL3.1600 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。