539648

Staurosporine, N-Benzoyl

A cell-permeable Staurosporine derivative that displays antitumor properties.

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₃₅H₃₀N₄O₄
• Número CAS: 120685-11-2
• Peso molecular: 570.64
• MDL number: MFCD00871372
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Propiedades

• Quality Segment: 100
• 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
• 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

Descripción

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).

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

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.

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Información de seguridad

• Pictogramas: GHS08
• Palabra de advertencia: Danger
• Códigos de peligro: H360FD
• Indicaciones de precaución: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Hazard Classifications: Repr. 1B
• Clase de almacenamiento: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• ¿Qué está pasando?: WGK 2
• Punto de inflamación (°F): Not applicable
• Punto de inflamación (°C): Not applicable