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.

Synthesis

GENERAL METHOD: 4-Chloro-6,7-dimethoxyquinazoline (1 mmol) was dissolved in refluxing 2-propanol (20 mL) and m-bromoaniline (1 mmol) was added dropwise. The reaction mixture was refluxed for 3-4 hours and the progress of the reaction was monitored by TLC until completion. Upon completion of the reaction, the precipitate was filtered out and washed sequentially with 2-propanol (10 mL) and ether (10 mL). If no precipitate formation was observed, the solvent was removed under reduced pressure to obtain a solid product. The final product was purified by recrystallization from 75% ethanol solution.

target

EGFR

References

[1] DAVID W. FRY. A Specific Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase[J]. Science, 1994, 265 5175. DOI:10.1126/science.8066447
[2] M BOS. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner.[J]. Clinical Cancer Research, 1997, 3 11: 2099-2106.
[3] MARIE-PIER TÉTREAULT. Specific signaling cascades involved in cell spreading during healing of micro-wounded gastric epithelial monolayers[J]. Journal of cellular biochemistry, 2008, 105 5: 1240-1249. DOI:10.1002/jcb.21924

PD 153035 HYDROCHLORIDE(153436-54-5)Related Product Information

• TCPOBOP
• TYRPHOSTIN AG 1296
• Cantharidin
• Brefeldin A
• (1-Bromoethyl)benzene
• 1-(2-BROMOPHENYL)-2-THIOUREA
• PD 153035 HYDROCHLORIDE
• JAK3 INHIBITOR II
• 4-(3',5'-DIBROMO-4-HYDROXYPHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINE
• 4-[(3-BROMOPHENYL)AMINO]-6,7-DIETHOXYQUINAZOLINE