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PD153035

Cat. No. M4850
PD153035 Structure
Synonym:

ZM 252868, AG 1517

Size Price Availability Quantity
10mM*1mL In DMSO USD 70 In stock
10mg USD 65 In stock
50mg USD 240 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

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 360.21
Formula C16H14BrN3O2
CAS Number 153436-54-5
Purity >99%
Solubility DMSO
Storage at -20°C
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
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References

Inhibitors of epidermoid growth factor receptor suppress cell growth and enhance chemosensitivity of nasopharyngeal cancer cells in vitro.
Hsu CH, et al. Oncology. 2005;68(4-6):538-47. PMID: 16037687.

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.
Bridges AJ, et al. J Med Chem. 1996 Jan 5;39(1):267-76. PMID: 8568816.

A specific inhibitor of the epidermal growth factor receptor tyrosine kinase.
Fry DW, et al. Science. 1994 Aug 19;265(5175):1093-5. PMID: 8066447.

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

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