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PP121

SKU: orb1227004

Description

A multitargeted, dual tyrosine and PI3K kinase inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2, 8, 10, 12, 14 and 18 nM; also inhibits Ret, VEGFR-2, 110α/mTOR, potently inhibits both tyrosine kinases and PI3Ks but not serine-threonine kinases.

Images & Validation

Key Properties

CAS Number1092788-83-4
MW319.3638
Purity>98% (HPLC)
FormulaC17H17N7
SMILESNC1=C2C(N(C3CCCC3)N=C2C4=CN=C(NC=C5)C5=C4)=NC=N1
TargetPI3K
Solubility10 mM in DMSO

Bioactivity

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.
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

PP 121 | PP-121

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PP121 (orb1227004)

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Available Sizes

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200 mg
500 mg
5 mg
¥ 1,300.00
10 mg
¥ 1,690.00
25 mg
¥ 2,990.00
50 mg
¥ 4,550.00
100 mg
¥ 6,500.00