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Merck
CN

234490

Sigma-Aldrich

PD 153035

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50 = 25 pM; Ki = 6 pM).

别名:

PD 153035, AG 1517, 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline, SU 5271, Compound 32

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关于此项目

经验公式（希尔记法）:
C16H14BrN3O2
化学文摘社编号:
153436-54-5
分子量:
360.21
MDL编号:
MFCD00934896
UNSPSC代码:
12352200
NACRES:
NA.77

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质量水平

100

方案

≥97% (HPLC)

表单

solid

效能

25 pM IC50

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

white

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

−20°C

SMILES字符串

Brc1cc(ccc1)Nc2ncnc3c2cc(c(c3)OC)OC

InChI

1S/C16H14BrN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)

InChI key

LSPANGZZENHZNJ-UHFFFAOYSA-N

相关类别

一般描述

An extremely potent, cell-permeamble, reversible, ATP-competitive and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50 = 25 pM; Ki = 6 pM). Rapidly suppresses autophosphorylation of EGFR at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells. Also selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. A 10 mM (500 µg/139 µl) solution of PD 153035 (Cat. No. 234491) in DMSO is also available.

生化/生理作用

Cell permeable: yes
Primary Target
EGFR
Product competes with ATP.
Reversible: yes
Target Ki: 6 pM against epidermal growth factor receptor (EGFR)

制备说明

Following reconstitution aliquot and freeze at -20°C. Stock solutions are stable for up to 6 months at -20°C.

其他说明

Bridges, A.J., et al. 1996. J. Med. Chem. 39, 267.
Fry, D.W., et al. 1994. Science265, 1093.

法律信息

Sold under license of U.S. Patent 5,457,105 and European Patent 0,566,266.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 1

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D W Fry et al.
Science (New York, N.Y.), 265(5175), 1093-1095 (1994-08-19)
A small molecule called PD 153035 inhibited the epidermal growth factor (EGF) receptor tyrosine kinase with a 5-pM inhibition constant. The inhibitor was specific for the EGF receptor tyrosine kinase and inhibited other purified tyrosine kinases only at micromolar or
A J Bridges et al.
Journal of medicinal chemistry, 39(1), 267-276 (1996-01-05)
4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (32, PD 153035) is a very potent inhibitor (IC50 0.025 nM) of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR), binding competitively at the ATP site. Structure-activity relationships for close analogues of 32 are very steep.
Gaurav Agrahari et al.
The Journal of investigative dermatology, 140(3), 656-665 (2019-08-30)
The expressions of LL-37 and KLK-5 were found to be altered in various dermatoses, including atopic dermatitis, psoriasis, and rosacea. However, the downstream inflammatory effect of LL-37 and KLK-5 is not as well studied. In addition, there is little high-quality
Albrecht Stenzinger et al.
Cells, tissues, organs, 184(2), 76-87 (2007-03-16)
The novel protein PTPIP51 (protein tyrosine phosphatase-interacting protein 51), which has been found to interact with protein tyrosine phosphatases of the PTP1B/TcPTP subfamily, is expressed in all suprabasal layers of human epidermis. Hence, a human keratinocyte cell line (HaCaT) grown
Laleh Abbassi et al.
Nature communications, 12(1), 1438-1438 (2021-03-06)
Germ cells are physically coupled to somatic support cells of the gonad during differentiation, but this coupling must be disrupted when they are mature, freeing them to participate in fertilization. In mammalian females, coupling occurs via specialized filopodia that project

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Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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