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. |
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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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(158.00 mM;Need ultrasonic) 配制储备液 | 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℃, 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。 |
