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Merck
CN

539648

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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关于此项目

经验公式（希尔记法）:
C35H30N4O4
化学文摘社编号:
120685-11-2
分子量:
570.64
MDL number:
MFCD00871372
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze
protect from light

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产品名称

Staurosporine, N-Benzoyl, A cell-permeable Staurosporine derivative that displays antitumor properties.

SMILES string

[n]21c3c4[n](c7c(c4c8c(c3c9c2cccc9)CNC8=O)cccc7)[C@@H]5O[C@]1([C@@]([C@@H]5N(C)C(=O)c6ccccc6)(OC)C)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 key

IIQIEMHSDLLZQA-QZPVEUDVSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

tan

solubility

DMSO: 6 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

相关类别

Biochem/physiol Actions

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

Disclaimer

Toxicity: Standard Handling (A)

General description

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).

Other Notes

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.

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

pictograms

Health hazard
GHS08

signalword

Danger

hcodes

H360FD

Hazard Classifications

Repr. 1B

存储类别

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

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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