PP121


CAS No. : 1092788-83-4

1092788-83-4
Price and Availability of CAS No. : 1092788-83-4
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10mg $90 In-stock
50mg $320 In-stock
100mg $395 In-stock
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Cat. No. : HY-10372
M.Wt: 319.36
Formula: C17H17N7
Purity: >98 %
Storage: at -20℃ 3 years
Solubility: DMSO
Introduction of 1092788-83-4 :

PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively. IC50 & Target: IC50: 10 nM (mTOR), 60 nM (DNK-PK), 12 nM (VEGFR2), 14 nM (Src), 2 nM (PDGFR)[1] In Vitro: PP121 blocks the PI3K pathway by direct inhibition of PI3K/mTOR in two glioblastoma cell lines, U87 and LN229. PP121 potently inhibits the proliferation of a diverse panel of tumor cell lines containing mutations in the PI3-K pathway components PIK3CA, PTEN, or RAS. PP121 induces a G0G1 arrest in most tumor cells. PP121 directly inhibits Src in cells and reverses its biochemical and morphological effects. PP121 potently inhibits the Ret kinase domain in vitro (IC50<1 nM). PP121 potently blocks VEGF stimulated activation of the PI3-K and MAPK pathways. PP121 inhibits VEGFR2 autophosphorylation at low nanomolar concentrations, confirming that this molecule directly targets VEGFR2 in cells. PP121 inhibits Bcr-Abl induced tyrosine phosphorylation in K562 cells as well as BaF3 cells that express Bcr-Abl[1]. In Vivo: Oral administration of PP121 remarkably inhibits Eca-109 xenograft growth. Mice body weights are not significantly affected by PP121 or the vehicle treatment. PP121 oral administration dramatically inhibits activations of Akt-mTOR and NFkB in xenograft tumors. p-Akt Ser 473 and p-IKKa/b are both inhibited by PP121 administration[2].

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