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PD153035 hydrochloride

Cat. No. M3689
PD153035 hydrochloride Structure
Synonym:

ZM 252868, AG 1517

Size Price Availability Quantity
10mg USD 66 In stock
50mg USD 250 In stock
100mg USD 420 In stock
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Quality Control
Biological Activity

PD153035 hydrochloride (ZM 252868, AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. PD153035 HCl 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. PD 153035 inhibits other purified tyrosine kinases only at micromolar or higher concentrations.

Protocol
Cell Experiment
Cell lines A431, Difi, DU145, MDA-MB-468 and ME180
Preparation method Seeding cells in sixwell plates. The next day, changing cells to medium containing 0.5% FBS for 18 hours, and then adding PD153035 at various concentrations to the cultures. After 72 hours of treatment, washing cells once with PBS, harvesting with 0.1% human trypsin-l mM EDTA in PBS, and counting with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.
Concentrations 0-3 μM
Incubation time 72 hours
Animal Experiment
Animal models A431 cells are injected into the outbred nude mice
Formulation PD153035 is dissolved in water.
Dosages ≤80 mg/kg
Administration Administered via i.p.
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 396.67
Formula C16H14BrN3O2.HCl
CAS Number 183322-45-4
Purity >99%
Solubility DMSO <1 mg/mL
Water <1 mg/mL
Ethanol <1 mg/mL
Storage at -20°C
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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  Catalog
Abmole Inhibitor Catalog 2017




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

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