PD153035 HCl Inhibitor CAS No. 183322-45-4

Cat. No.	Name	Size	Price
KI1436	PD153035 HCl	10 mg	$280
	PD153035 HCl	50 mg	$1120
	PD153035 HCl	200 mg	$3584

Chemical Characteristic

Product Name	PD153035 HCl
CAS No.	183322-45-4
Molecular Weight	396.67
Formula	C₁₆H₁₄BrN₃O₂.HCl
Chemical Name	6,7-Dimethoxy-4-[N-(3-bromophenyl)amino]quinazoline hydrochloride
Smiles	n1cnc(c2cc(c(cc12)OC)OC)Nc1cc(ccc1)Br Cl
Chemical Structure

Biological activities

PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase. PD153035 inhibits the EGF receptor tyrosine kinase with an IC50 of 29 pM. PD153035 inhibits the EGF receptor with a Ki of 5 pM.^[1] PD153035 inhibits EGF-dependent EGF receptor phosphorylation and suppresses the proliferation and clonogenicity of a wide panel of EGF receptor-overexpressing human cancer cell lines. PD153035 reduces heregulin-dependent tyrosine phosphorylation in HER2/neu-overexpressing cell lines at significantly higher concentrations (1.4-2.8 mM). PD153035 causes a dose-dependent growth inhibition of EGF receptor- overexpressing cell lines with an IC50 less than 1 mM. PD153053 also abolishes all growth effects mediated by the addition of exogenous EGF. ^[2] PD153035 causes a rapid reduction in EGF receptor phosphorylation and a concomitant reduction in EGF-stimulated receptor tyrosine kinase activity. PD153035 suppresses phosphorylation of the EGF receptor in A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice.^[3] PD153035 treatment for 1 day decreases the protein expression of inducible nitric oxide synthase, tumor necrosis factor (TNF)-α, and interleukin (IL)-6 in the stroma vascular fraction. PD153035 reduces JNK and IKK/IκB/NF-κB pathways. Treatment with PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. ^[4]

Protocols

PD153035 is prepared in water. ^[3]

References

[1] Fredriksson A, et al. In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants. Life Sci. 1999, 65(2): 165-174. [2] Bos M, et al. 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. 1997, 3(11): 2099-2106. [3] Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996, 13(4): 295-302. [4] Prada PO, et al. EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice. Diabetes. 2009, 58(12): 2910-2919.

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