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PD153035

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Catalog No. T2041Cas No. 153436-54-5
Alias ZM 252868, SU-5271, NSC 669364, AG1517

PD153035 (NSC-669364) hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.

PD153035

PD153035

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🥰Excellent
Purity: 99.29%
Catalog No. T2041Alias ZM 252868, SU-5271, NSC 669364, AG1517Cas No. 153436-54-5
PD153035 (NSC-669364) hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$35In StockIn Stock
25 mg$73In StockIn Stock
50 mg$135In StockIn Stock
100 mg$236In StockIn Stock
200 mg$353In StockIn Stock
1 mL x 10 mM (in DMSO)$34In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.29%
Appearance:Solid
Color:White
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Product Introduction

PD153035 AI Summary
PD153035 demonstrates significant bioactivity as a potent inhibitor of the Epidermal Growth Factor Receptor (EGFR) tyrosine kinase activity with an exceptionally low IC50 value of 0.025 nM. This compound also inhibits the phosphorylation of phospholipase C-gamma1 by EGFR at the same IC50 value, highlighting its strong affinity for EGFR. Additionally, PD153035 shows inhibitory activity against other kinases such as v-Abl tyrosine kinase and c-Src tyrosine kinase, with varying efficacy. It also exhibits antiproliferative effects on various cancer cell lines, including human A431 cells, with IC50 values ranging from nanomolar to micromolar concentrations. Furthermore, it demonstrates a broad spectrum of activity against other targets, such as fructose-1,6-bisphosphatase and MNK1 kinase, and it possesses cytotoxic properties in specific cancer cell lines. These findings highlight PD153035's potential as a therapeutic candidate for EGFR-related diseases and cancer treatment..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
PD153035 (NSC-669364) hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.
Targets&IC50
EGFR:29 pM
SynonymsZM 252868, SU-5271, NSC 669364, AG1517
Chemical Properties
Molecular Weight360.21
FormulaC16H14BrN3O2
Cas No.153436-54-5
SmilesCOC1=CC2=NC=NC(NC3=CC(Br)=CC=C3)=C2C=C1OC
Relative Density.1.499 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 5 mg/mL (13.88 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7762 mL13.8808 mL27.7616 mL138.8079 mL
5 mM0.5552 mL2.7762 mL5.5523 mL27.7616 mL
10 mM0.2776 mL1.3881 mL2.7762 mL13.8808 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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