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Merck
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文件

539648

Sigma-Aldrich

Staurosporine, N-Benzoyl

A cell-permeable Staurosporine derivative that displays antitumor properties.

别名:

Staurosporine, N-Benzoyl, PKG Inhibitor IX, N-Benzoylstaurosporine, CGP 41 251, PDGFR Tyrosine Kinase Inhibitor X, PKC412, PKG Inhibitor IX, N-Benzoylstaurosporine, CGP 41 251, PKC412, PDGFR Tyrosine Kinase Inhibitor X

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About This Item

经验公式(希尔记法):
C35H30N4O4
分子量:
570.64
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

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

tan

溶解度

DMSO: 6 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

InChI

1S/C35H30N4O4/c1-34(42-4)30(37(3)32(41)19-12-6-5-7-13-19)33-38-23-16-10-8-14-20(23)26-27-22(18-36-31(27)40)25-21-15-9-11-17-24(21)39(29(25)28(26)38)35(34,2)43-33/h5-17,30,33H,18H2,1-4H3,(H,36,40)/t30-,33-,34-,35+/m1/s1

InChI 密鑰

IIQIEMHSDLLZQA-QZPVEUDVSA-N

一般說明

A cell-permeable Staurosporine (Cat. No. 569397) derivative that displays antitumor properties. Acts as a broad-spectrum, reversible, and ATP-competitive inhibitor of PKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR (IC50 = 22 nM, 50 nM, 86 nM, 95 nM, 160 nM, 330 nM, 390 nM, 528 nM, 570 nM, 570 nM, 600 nM, 790 nM, 800 nM, 912 nM, and 1.0 µM, respectively). At higher concentrations, also inhibits Ins-R and IGF-1R (IC50 = 10 &microM). Shown to potently inhibit the proliferation of Ba/F3 cells expressing constitutively active Flt3 (IC50<10 nM).

生化/生理作用

Cell permeable: yes
Primary Target
PKC (α, β and γ), PDGFRβ, VEGFR2, Syk, PKCη, PKCδ, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, and EGFR
Product competes with ATP.
Reversible: yes
Target IC50: 22 nM, 50 nM, 86 nM, 95 nM, 160 nM, 330 nM, 390 nM, 528 nM, 570 nM, 570 nM, 600 nM, 790 nM, 800 nM, 912 nM, and 1.0 µM against primary targets in the order listed

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

Weisberg, E., et al. 2002. Cancer Cell1, 433.
Fabbro, D., et al. 2000. Anticancer Drug Des.15, 17.
Meyer, T., et al. 1999. Int. J. Cancer81, 669.
Meyer, T., et al. 1989. Int. J. Cancer43, 851.

法律資訊

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

象形圖

Health hazard

訊號詞

Danger

危險聲明

危險分類

Repr. 1B

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 2

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Scientific reports, 12(1), 13796-13796 (2022-08-14)
Therapeutic resistance to kinase inhibitors constitutes a major unresolved clinical challenge in cancer and especially in glioblastoma. Multi-kinase inhibitors may be used for simultaneous targeting of multiple target kinases and thereby potentially overcome kinase inhibitor resistance. However, in most cases

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