539652

PKC_βII/EGFR Inhibitor

The PKC_βII/EGFR Inhibitor, also referenced under CAS 145915-60-2, controls the biological activity of PKC_βII/EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 同義詞: PKC_βII/EGFR Inhibitor, CG53353, DAPH 2, 4,5-bis(4-Fluoroanilino)-phthalimide, CGP 53 353
• 經驗公式（希爾表示法）: C₂₀H₁₃F₂N₃O₂
• CAS號碼: 145915-60-2
• 分子量：: 365.33
• MDL號碼: MFCD00938569
• 分類程式碼代碼: 12352200

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: orange
• 溶解度: DMSO: 20 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• InChI: 1S/C20H13F2N3O2/c21-11-1-5-13(6-2-11)23-17-9-15-16(20(27)25-19(15)26)10-18(17)24-14-7-3-12(22)4-8-14/h1-10,23-24H,(H,25,26,27)
• InChI 密鑰: RONQPWQYDRPRGG-UHFFFAOYSA-N

描述

一般說明

A cell-permeable symmetrical phthalimide compound that acts as a potent, reversible, and ATP-competitive inhibitor of EGFR and PKC isozymes α, βI, and βII (IC₅₀ = 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM, respectively). Only weakly inhibits the activity of a panel of 16 other kinases, including novel and atypical PKC isozymes. Reported to inhibit insulin-stimulated cellular 2-deoxyglucose uptake, osteoclast differentiation, ERK activation, and TLS/FUS DNA-binding activity in vitro. Also reported to exhibit antitumor activity in mice in vivo.

生化／生理作用

Cell permeable: yes

Primary Target
EGFR

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.7 µM, 1.9 µM, 3.8 µM, and 0.41 µM against EGFR and PKC isozymes α, βI, and βII, respectively

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

Kouroedov, A., et al. 2004. Circulation110, 91.
Lee, S.W., et al. 2003. Bone32, 217.
Perrotti, D., et al. 1998. EMBO J.17, 4442.
Chalfant, C.E., et al. 1996. Mol. Endocrinol.10, 1273.
Buchdunger, E., et al. 1995. Clin. Cancer Res.1, 813.
Trinks, U., et al. 1994. J. Med. Chem.37, 1015.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable