Name: PD 153035
Brand: Alomone Labs
SKU: P-360

Cat #: P-360

Lyophilized Powder yes

Bioassay Tested

Source Synthetic

MW: 360.21

Purity: >99%

Effective concentration 10-500 nM.

Structure

Chemical name 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline.

Molecular formula C₁₆H₁₄BrN₃O₂.

CAS No.: 153436-54-5

Activity PD 153035 is a potent inhibitor of the epidermal growth factor receptor (EGFR), (IC₅₀ = 50 pM)¹.

References-Activity

Fry, D. et al. (1994) Science 2665, 1093.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO or ethanol. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to two weeks at 4°C or six months at -20°C.

Our bioassay

Alomone Labs PD 153035 inhibits EGF receptor activation in 3T3-L1 cells.
Cells were serum starved for 3 h and preincubated with different concentrations of PD 153035 (#P-360) for 2 h. The cells were then stimulated with 200 ng/ml EGF for 10 minutes. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-EGFr (upper panel) and with anti-phospho ERK1/2 (lower panel).

References - Scientific background

Fry, D.W. et al. (1994) Science 265, 1093.
Kunkel, M.W. et al. (1996) Invest. New Drugs 13, 295.
Bridges, A.J. et al. (1996) J. Med. Chem. 39, 267.
Bos, M. et al. (1997) Clin. Cancer Res. 3, 2099.
Goossens, J.F. et al. (2001) Biochemistry 40, 4663.
Faust, R.A. et al. (1999) Oral Oncol. 35 290.
Kunkel, M.W. et al. (1996) Invest New Drugs, 13. 295.
Fredriksson, A. et al. (1999) Life Sci. 65, 165.

Scientific background

PD 153035 is a small molecule derived from brominated anilinoquinazoline which inhibits tyrosine kinase activity of the EGFR by competition at the ATP binding site. PD 153035 is a highly potent inhibitor for auto and hetro tyrosine kinase activity of EGF receptor (ERB2) at sub nM concentrations and inhibits other purified tyrosine kinases only at micromolar or higher concentrations.^1-3

PD 153053 abolished all growth effects mediated by the addition of exogenous EGF in a receptor number-dependent manner and shows a remarkable apoptotic and cytotoxic activity against several types of tumor cell lines that overexpress the EGF receptor in vitro and in vivo .^4-8

Lyophilized Powder

Last update: 13/10/2022

PD 153035 (#P-360) is a highly pure, synthetic, and biologically active compound.

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PD 153035

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