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Merck
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資料

安全性情報

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).

別名:

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

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About This Item

実験式（ヒル表記法）:
C16H14BrN3O2
CAS番号:
153436-54-5
分子量:
360.21
UNSPSCコード:
12352200
NACRES:
NA.77

品質水準

100

アッセイ

≥97% (HPLC)

形状

solid

有効性

25 pM IC50

メーカー／製品名

Calbiochem®

保管条件

OK to freeze
protect from light

色

white

溶解性

DMSO: 5 mg/mL

輸送温度

ambient

保管温度

−20°C

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

詳細

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.
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.

生物化学的／生理学的作用

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

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 1

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

234490-1.1ML:
234490-1MG:
234490-VUG:

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

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.
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
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
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
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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