产品描述: | 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 |
靶点: |
IC50: 10 μM (TrKA phosphorylation) IC50: 1 μM (ErbB2);Apoptosis; EGFR; Trkreceptor; HER; PDGFR |
体内研究: |
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 |
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 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. |
溶解性: |
DMSO : 50 mg/mL (158.00 mM; Need ultrasonic) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.16 ml |
15.8 ml |
31.6 ml |
5 mM |
0.632 ml |
3.16 ml |
6.32 ml |
10 mM |
0.316 ml |
1.58 ml |
3.16 ml |
50 mM |
0.063 ml |
0.316 ml |
0.632 ml |
|
注意: |
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