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PD153035

Cat. No. M4850
PD153035 Structure
Synonym:

ZM 252868, AG 1517

Size Price Availability Quantity
10mM*1mL USD 70  USD70 In stock
10mg USD 80  USD80 In stock
50mg USD 310  USD310 In stock
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Quality Control & Documentation
Biological Activity

PD153035(ZM 252868, AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. PD153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells,respectively.PD153035 induces a dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC) cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of 12.9 μM, 9.8 μM and 18.6μM, respectively. PD153035 inhibits other purified tyrosine kinases only at micromolar or higher concentrations.

Customer Product Validations & Biological Datas
Source Chem Biol Interact (2016). Figure 6. PD153035
Method EdU Labeling
Cell Lines NHEKs
Concentrations 300 nM
Incubation Time 72 h
Results To address this question, we measured DNA synthesis using EdU labeling in cells treated for 72 h with TCDD in the presence or absence of the EGFR inhibitor PD153035 (300 nM). Compared to basal cells, TCDD treatment significantly increased the percentage of the cell population that was proliferating
Chemical Information
Molecular Weight 360.21
Formula C16H14BrN3O2
CAS Number 153436-54-5
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Hsu CH, et al. Oncology. Inhibitors of epidermoid growth factor receptor suppress cell growth and enhance chemosensitivity of nasopharyngeal cancer cells in vitro.

[2] Bridges AJ, et al. J Med Chem. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.

[3] Fry DW, et al. Science. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase.

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Keywords: PD153035, ZM 252868, AG 1517 supplier, EGFR/HER2, inhibitors, activators


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