539648

Staurosporine, N-Benzoyl

A cell-permeable Staurosporine derivative that displays antitumor properties.

• Synonyme(s) : 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
• Formule empirique (notation de Hill): C₃₅H₃₀N₄O₄
• Numéro CAS: 120685-11-2
• Poids moléculaire : 570.64
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: tan
• Solubilité: DMSO: 6 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −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
• Clé InChI: IIQIEMHSDLLZQA-QZPVEUDVSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Pictogrammes: GHS08
• Mention d'avertissement: Danger
• Mentions de danger: H360FD
• Conseils de prudence: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Classification des risques: Repr. 1B
• Code de la classe de stockage: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable