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Tyrosine Kinase/Adaptors Hck PP121

PP121

Catalog No. T2415   CAS 1092788-83-4

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

PP121, CAS 1092788-83-4
Pack Size Availability Price/USD Quantity
5 mg In stock 57.00
10 mg In stock 87.00
25 mg In stock 174.00
50 mg In stock 285.00
100 mg In stock 404.00
1 mL * 10 mM (in DMSO) In stock 57.00
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Purity 99.67%
Purity 99.19%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
Targets&IC50 Hck : ic50 8nM ,   mTOR : ic50 13nM ,   PDGFR : ic50 2nM ,   Src : ic50 14nM ,   VEGFR : ic50 12nM ,   Abl
Kinase Assay Kinase assays: Purified kinase domains are incubated with PP-121 at 2- or 4-fold dilutions over a concentration range of 1nM-50 µM or with vehicle (0.1% DMSO) in the presence of 10 µM ATP, 2.5 µCi of γ-32P-ATP and substrate. Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes, depending on the substrate; this membrane is then washed 5–6 times to remove unbound radioactivity and dried. Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software.
Cell Research
For western blot analysis, cells are grown in 12-well plates and treated with PP-121 at the indicated concentrations or vehicle (0.1% DMSO). Treated cells are lysed, lysates are resolved by SDS-PAGE, transferred to nitrocellulose and blotted. For cell proliferation assays,cells are grown in 96-well plates are treated with PP-121 at 4-fold dilutions (10 µM - 0.040 μM) or vehicle (0.1% DMSO). After 72 hours cells are exposed to Resazurin sodium salt (22 µM) and fluorescence is quantified. IC50 values are calculated using Prism software. For proliferation assays involving single cell counting, non-adherent cells are plated at low density (3–5% confluence) and treated with PP-121 (2.5 µM) or vehicle (0.1% DMSO). Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer. For apoptosis and cell cycle analysis, cells are treated with the indicated concentration of PP-121 or vehicle (0.1% DMSO) for 24–72 hours. Cells are either stained live with AnnexinV-FITC or fixed with ethanol and stained with propidium iodide. Cell populations are separated using a FacsCalibur flow cytometer; data is collected using CellQuest Pro software and analyzed with either ModFit or FlowJo Software.(Only for Reference)
Cell lines: U87, LN229, NIH3T3, HUVECs, BaF3 and TT thyroid carcinoma cells
Molecular Weight 319.36
Formula C17H17N7
CAS No. 1092788-83-4

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 60 mg/mL (187.9 mM)

Ethanol: 2 mg/mL (6.26 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Apsel B, et al. Nat Chem Biol, 2008, 4(11), 691-699. 2. Peng Y, et al. The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Autophagy Compound Library PI3K-AKT-mTOR Compound Library Tyrosine kinase inhibitor library DNA Damage & Repair Compound Library Cytokine Inhibitor Library Kinase Inhibitor Library Angiogenesis related Compound Library

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