PP2(AGL 1879)

Cas No.:	172889-27-9
Chemical Name:	1-(tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Synonyms:	PP 2; AG1879
SMILES:	C1=NC(N)=C2C(C3=CC=C(Cl)C=C3)=NN(C(C)(C)C)C2=N1
Formula:	C15H16ClN5
M.Wt:	301.77
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
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].
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 IC50 of ~5 nM in vitro, concentrations to 10 μM are often necessary to achieve complete Src family kinase inhibition in cell culture[3].