Equivalent to the IC50 for wild-type PI3K¦Á, PKI-402 inhibits E545K and H1047R PI3K¦Á mutants with IC50 of 3 nM. In a panel of 236 human protein kinases, PKI-402 only displays inhibitory activity against C-Raf and B-Raf with IC50 of 7 ¦ÌM, and displays little activity against all other kinases with IC50 of > 10 ¦ÌM. PKI-402 inhibits the growth of human tumor cell lines with IC50 of 6-349 nM. Consistently, PKI-402 inhibits phosphorylation of PI3K and mTOR effector proteins, particularly phosphorylated Akt (p-Akt) at T308 and S473 with IC50 of <10 nM and <30 nM, respectively. PKI-402 inhibits both p70S6K and 4EBP1 phosphorylation with IC50 of <10 nM. PKI-402 inhibits Akt phosphorylation of PRAS40 at T246 with IC50 of <30 nM, and inhibits Akt phosphorylation of ENOS at S1177 and GSK3¦Á/GSK3¦Â at S9/S21 with IC50 of <10 nM. In MDAMB-361, a breast tumor line with mutant PI3K-¦Á (E545K) and elevated levels of Her2 receptor, PKI-402 treatment induces cleaved poly(ADP-ribose) polymerase (PARP), a marker for apoptosis. Less than 10% of MDAMB-361 cells exposed to PKI-402 at 0.3 ¦ÌM (or higher) for 24 hours remain viable.

June 21, 2017

prudect name : Equivalent to the IC50 for wild-type PI3K¦Á, PKI-402 inhibits E545K and H1047R PI3K¦Á mutants with IC50 of 3 nM. In a panel of 236 human protein kinases, PKI-402 only displays inhibitory activity against C-Raf and B-Raf with IC50 of 7 ¦ÌM, and displays little activity against all other kinases with IC50 of > 10 ¦ÌM. PKI-402 inhibits the growth of human tumor cell lines with IC50 of 6-349 nM. Consistently, PKI-402 inhibits phosphorylation of PI3K and mTOR effector proteins, particularly phosphorylated Akt (p-Akt) at T308 and S473 with IC50 of <10 nM and <30 nM, respectively. PKI-402 inhibits both p70S6K and 4EBP1 phosphorylation with IC50 of <10 nM. PKI-402 inhibits Akt phosphorylation of PRAS40 at T246 with IC50 of <30 nM, and inhibits Akt phosphorylation of ENOS at S1177 and GSK3¦Á/GSK3¦Â at S9/S21 with IC50 of <10 nM. In MDAMB-361, a breast tumor line with mutant PI3K-¦Á (E545K) and elevated levels of Her2 receptor, PKI-402 treatment induces cleaved poly(ADP-ribose) polymerase (PARP), a marker for apoptosis. Less than 10% of MDAMB-361 cells exposed to PKI-402 at 0.3 ¦ÌM (or higher) for 24 hours remain viable.
PKI 402

Synonyms: CAS NO: 1173204-81-3Molecular Formula: C₂₉H₃₄N₁₀O₃Molecular Weight: 570.65Purity: 98% minSolubility: In DMSOStorage: -20°C

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