>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

PP2 AGL 1879

PP2 (AG 1879, AGL 1879) 是一种Src家族激酶抑制剂，有效抑制Lck/Fyn，无细胞试验中IC50为4 nM/5 nM，作用于EGFR效果低100倍左右，对ZAP-70，JAK2和PKA没有活性。

货号：
TK0396
规格：

2mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	172889-27-9
生物活性	PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
分子式	C15H16ClN5
分子量	301.77
储存条件	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶解性数据	DMSO : 50 mg/mL (165.69 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
体内研究	The tumor growth inhibition rate is 25% in the PP2 treatment group and 5% in the Gemcitabine treatment group (P>0.05). When administered in combination, PP2 and Gemcitabine produce a tumor growth inhibition rate of 98% (P<0.05). Hepatic metastasis occurred in 100% of control and Gemcitabine-treated groups; 88% of the PP2-treated group developed liver metastases. There are no detectable metastases in the group treated with PP2 and Gemcitabine in combination (P<0.05).
体外研究	At 10 μM, the effect of PP2 on cellular proliferation is not significant, indicating that, at this low concentration, the effect of PP2 on Gemcitabine cytotoxicity does not simply reflect a direct antiproliferative effect, but rather a potentiation of Gemcitabine-induced cytotoxicity. Above 20 μM, growth is increasingly suppressed, a finding consistent with reports in other human cancer cell lines. Although 10 μM PP2 is used in our study, at higher concentrations PP2 is reported to inhibit other intracellular kinases. PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50 of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture.

推荐产品