Description
PP121 can inhibit a list of kinases including PDGFR, Hck, mTOR, VEGFR2, Src, bcr-Abl, p110alpha, DNA-PK, p110delta, EphB4, Src(T338I), EGFR, p110gamma, p110beta with IC50 of 2nM, 8nM, 10nM, 12nM, 14nM, 18nM, 52nM, 60nM, 150nM, 190nM, 220nM, 260nM, 110nM, 1400nM.
Storage
2 years at -20 centigrade
Targets
PDGFR, Hck, mTOR, VEGFR2, Src
Molecular Formula
C17H17N7
Chemical Name
1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Solubility
DSMO 64 mg/mL Water
In vitro
PP121 can inhibit a list of kinases including PDGFR, Hck, mTOR, VEGFR2, Src, bcr-Abl, p110alpha, DNA-PK, p110delta, EphB4, Src(T338I), EGFR, p110gamma, p110beta with IC50 of 2nM, 8nM, 10nM, 12nM, 14nM, 18nM, 52nM, 60nM, 150nM, 190nM, 220nM, 260nM, 110nM, 1400nM. Actually, PP121 can potently inhibit both tyrosine kinases and PI3-Ks but not serine-threonine kinases. And PP121 also shows inhibition to tube formation. Actually, PP121 potently blocked tube formation with IC50 of 0.31 nM. PP121 potently and dose-dependently blocked the phosphorylation of Akt, p70S6K and S6 in U87 and LN229, both of which are glioblastoma cell lines. Because of the PTEN feedback loop existing in U87, PP121 shows more potent inhibition to LN229 than U87. Actually, PP121 directly inhibit kinases such as PI3K and mTOR to block PI3K signaling pathway rather than inhibit upstream RTKs, so that PP121 shows little inhibition to ERK until 10 uM.PP121 potently inhibited the proliferation of a subset of these lines, and the inhibition of PP121 is as potent as that of PP103. PP121 induced a G0G1 arrest in most tumor cells. PP121 can override resistance in CML by inhibiting Abl, PI3K and mTOR at the same time.
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