PD 153035 HYDROCHLORIDE

Synonym(s):4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline hydrochloride;AG 1517;PD 153035;SU 5271;ZM 252868

CAS NO.：153436-54-5
Empirical Formula: C16H14BrN3O2
Molecular Weight: 360.21
MDL number: MFCD00934896
SAFETY DATA SHEET (SDS)
Update Date: 2024-11-19 20:33:22

What is PD 153035 HYDROCHLORIDE?

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

The Uses of PD 153035 HYDROCHLORIDE

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

The Uses of PD 153035 HYDROCHLORIDE

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

What are the applications of Application

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

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.

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

Properties of PD 153035 HYDROCHLORIDE

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.

Safety information for PD 153035 HYDROCHLORIDE

Signal word	Warning
Pictogram(s)	Exclamation Mark Irritant GHS07
GHS Hazard Statements	H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H332:Acute toxicity,inhalation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes	P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.