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PP242MTOR inhibitor, selective and ATP-competitive

PP242

Catalog No. A8318
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $50.00 In stock
25mg $150.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

PP242

Related Biological Data

PP242

Related Biological Data

PP242

Biological Activity

Description PP242 is a selective inhibitor of mTOR with IC50 of 8 nM.
Targets mTOR          
IC50 8 nM          

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Chemical Properties

Cas No. 1092351-67-1 SDF Download SDF
Synonyms PP242; PP-242
Chemical Name (2E)-2-(4-amino-1-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-3-ylidene)indol-5-ol
Canonical SMILES CC(C)N1C2=C(C(=C3C=C4C=C(C=CC4=N3)O)N1)C(=NC=N2)N
Formula C16H16N6O M.Wt 308.35
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PP242, a novel potent and selective mTOR inhibitor, can inhibit the active site of mTOR kinase in both mTORC1 and mTORC2 with IC50 of 8 nM.
The mammalian target of rapamycin (mTOR), a serine-threonine kinase, is present in two protein complexes, mTORC1 and mTORC2, that have distinct subunit composition, substrates and mechanisms of activation.
Treatment of PP242 was shown to lead to the death of certain mouse and human leukemia cells [1]. In primary AML cells and CD34+ progenitor cells, PP242 can inhibit the activity of mTOR and their downstream targets, therefore inducing cell apoptosis [2].
The component has also been used to study the role of COX-2 in vivo. In models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation, PP242 can delay the onset of leukemia and augment the effects of front-line tyrosine kinase inhibitors more effectively, thereby suppressing the expansion of leukemia [1]. In addition, PP242 was shown to suppresse leukemia progression in a murine leukemia model which was driven by mutated FLT3 with constitutive activation of mTOR [2].
References:
1.Janes MR, Limon JJ, So L, Chen J, Lim RJ, Chavez MA, et al. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med 2010,16:205-213.
2.Zeng Z, Shi YX, Tsao T, Qiu Y, Kornblau SM, Baggerly KA, et al. Targeting of mTORC1/2 by the mTOR kinase inhibitor PP242 induces apoptosis in AML cells under conditions mimicking the bone marrow microenvironment. Blood 2012,120:2679-2689.