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PP121

Cat. No. M2011
PP121 Structure
Size Price Availability Quantity
10mg USD 105 In stock
50mg USD 360 In stock
100mg USD 520 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR). PP121 is the first inhibitor active on both Tyrosine kinases and the phosphatidylinositol-3-OH kinase (PI(3)K) family. PP121 blocks the proliferation of tumor cells by direct inhibition of PI 3-K, mTOR, Src and the VEGF receptor. PP-121 induces a G0/G1 arrest in LN220, U87 and Seg1 cells. PP-121 directly inhibits Bcr-Abl induced tyrosine phosphorylation, resulting in drug-induced apoptosis in K562 cells and a combination of apoptosis and cell cycle arrest in Bcr-Abl expressing BaF3 cells. PP-121 also inhibits other PI3Ks including p110α and DNA-PK with IC50 of 52 nM and 60 nM, respectively.

Protocol
Cell Experiment
Cell lines U87 and LN229 cells line
Preparation method Cell proliferation assays.
Cells grown in 96-well plates were treated with inhibitor at 4-fold dilutions (10 µM - 0.040 μM) or vehicle (0.1% DMSO). After 72 h cells were exposed to Resazurin sodium salt (22 µM, Sigma) and fluorescence was quantified. IC50 values were calculated using Prism software. For proliferation assays involving single cell counting, non-adherent cells were plated at low density (3–5% confluence) and treated with drug (2.5 µM) or vehicle (0.1% DMSO). Cells were diluted into trypan blue daily and viable cells counted using a hemocytometer.
Concentrations 10 µM - 0.040 μM
Incubation time 72 h
Animal Experiment
Animal models Eca-109 cells Mice xenograft
Formulation 10% 1-methyl-2-pyrrolidinone and 90% PEG 300
Dosages 30 mg/kg daily for 30 days
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 319.36
Formula C17H17N7
CAS Number 1092788-83-4
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121.
Peng Y, et al. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44. PMID: 26235881.

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel B, et al. Nat Chem Biol. 2008 Nov;4(11):691-9. PMID: 18849971.

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  Catalog
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Keywords: PP121 supplier, VEGFR/PDGFR, inhibitors

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