PD 153035 HYDROCHLORIDE Chemical Properties

Melting point:

189-190 °C

Boiling point:

472.1±45.0 °C(Predicted)

Density 

1.499±0.06 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,2-8°C

solubility 

Soluble in DMSO (up to 5 mg/ml).

form 

White to off-white solid.

pka

5.55±0.30(Predicted)

color 

White or off-white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

PD 153035 HYDROCHLORIDE Usage And Synthesis

Description

AG-1517 HCl (153436-54-5) is an ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR), with an IC50 of 25 pM. Inhibits other tyrosine kinases at micromolar or higher concentrations. It selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression and oncogenic transformation.1?Inhibits the growth of a number of cancer cell lines.2?AG-1517 HCl is an extremely useful tool for exploring EGF-mediated cellular signaling.3

Chemical Properties

Yellowish solid

Uses

PD 153035 is an extremely potent and specific inhibitor of EGFR tyrosine kinase activity.

Uses

PD153035 is an inhibitor of EGFR, competitive with ATP. EGF Receptor: IC50 = 25 pM (Ki = 6 pM).

Definition

ChEBI: A member of the class of quinazolines carrying a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7.

Biological Activity

An extremely potent inhibitor of epidermal growth factor (EGF) receptor tyrosine kinase, with an IC 50 of 25 pM. Inhibits other purified tyrosine kinases only at micromolar or higher concentrations.

target

EGFR

References

1) Fry et al. (1994), A specific inhibitor of the epidermal growth factor receptor tyrosine kinase; Science, 265 1093 2) Bos et al. (1997), PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner; Clin. Cancer Res., 3 2099 3) Tetreault et al. (2008), Specific signaling cascades involved in cell spreading during healing of micro-wounded gastric epithelial monolayers; J. Cell. Biochem., 105 1240

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