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Datasheet of PP242

Description:.
PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for
mTOR than PI3K or PI3K//, respectively; also showed slightly weaker activity against BRD4 (Kd= 1.7 uM).
in vitro: PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110, p110, p110, p110, and
DNA-PK with IC50 of 1.96 M, 2.2 M, 1.27 M, 0.102 M, and 0.408 M, respectively. PP242 displays some inhibitory
activity against Ret, PKC, PKC, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike
rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 M) inhibits the
phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. The p38
inhibitor SB-202190 and the PI3K inhibitor PP-242 showed slightly weaker activity (Kd values: 3.4 0.13 M and 1.7 0.076
M, respectively) [2]. PP242 potently inhibits PKC with IC50 of 49 nM. Low concentrations of PP242 inhibit the
phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more
effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of
4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation,
by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin.
in vivo: Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of
mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the
phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6. PP242 treatment potently
inhibits the growth of 8226 cells in mice..

Chemical Information
Catalog

DC7482

Purity of current batch:

>98%

Molecular Weight (MW)

308.34

Molecular Formula

C16H16N6O

CAS No.

1092351-67-1

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.