CAS NO: | 172889-27-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | PP2 is a reversible and ATP-competitiveSrcfamily kinases inhibitor withIC50s of 4 and 5 nM forLckandFyn, respectively. | ||||||||||||||||
IC50& Target | IC50: 4 nM (Lck), 5 nM (Fyn)[1] | ||||||||||||||||
体外研究 (In Vitro) | 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[2]. PP2 is the most widely used commercially available Src family kinase inhibitor. PP2 inhibits Src family kinase activity with IC50of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture[3]. | ||||||||||||||||
体内研究 (In Vivo) | 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)[2]. | ||||||||||||||||
分子量 | 301.77 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C15H16ClN5 | ||||||||||||||||
CAS 号 | 172889-27-9 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(165.69 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液
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