PP242（mTOR inhibitor）

Biological Activity

...........................................................................................................................................................................................................................................

PP242 is a novel and specific mTOR kinase domain inhibitor (TORKinib) that ATP-competitively and potently targets mTOR (IC₅₀ = 8 nM), but showing much less activity against other PI3K family members.Unlike Rapamycin, PP242 inhibits both mTORC₁ and mTORC₂, therefore can be used to explore signaling by mTORC₂. PP242 demonstrates to be more effective than Rapamycin for mTORC₁ and also for the proliferation of primary cells. PP242 suppresses the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in BT549 cells ^[1-2]. PP242 induces death of established Ph(+) transformed leukemia cells more effectively than normal lymphocytes. PP242 enhances the efficacy of dasatinib and the combination causes regression of human Ph+ B-ALL xenografts. All results provide evidence for its development as a promising agent of leukemia therapy ^[3]. PP242 shows higher inhibitory effects than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma (MM) cells. Combining bortezomib with PP242 lead to synergistic anti-MM effects ^[4]. PP242 enhances HDAC inhibitor such as SAHA mediated anti-tumor efficacy in primary hepatocellular carcinoma (HCC) cancer in vitro and in vivo ^[5].

Chemical Properties

Cas No.: 1092351-67-1	M. Wt.: 308.34
Formula: C16H16N6O	Purity: >98.5% (HPLC)
Synonym: TORKinib (In some cases)
Chemical Name: 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
Appearance: White to off-white solid
Solubility: Soluble in DMSO at 35 mg/ml, very poorly soluble in water.
Storage: Store solid at -20 ºC for the stability of 2 years.

Application Concentration (Just for reference)

The appropriate working concentration of PP242 depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.