Title: Midostaurin
CAS Registry Number: 120685-11-2
CAS Name: N-[(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3¢,2¢,1¢-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methylbenzamide
Additional Names: N-benzoylstaurosporine
Manufacturers' Codes: CGP-41251; PKC-412
Molecular Formula: C35H30N4O4
Molecular Weight: 570.64
Percent Composition: C 73.67%, H 5.30%, N 9.82%, O 11.22%
Literature References: Protein kinase C inhibitor; derivative of the naturally occurring alkaloid, staurosporine, q.v. Prepn: G. Caravatti, A. Fredenhagen, EP 296110; eidem, US 5093330 (1988, 1992 both to Ciba-Geigy); G. Caravatti et al., Bioorg. Med. Chem. Lett. 4, 399 (1994). HPLC determn in plasma: R. van Gijn et al., J. Chromatogr. B 667, 269 (1995). Review of pharmacology: D. Fabbro et al., Pharmacol. Ther. 82, 293-301 (1999); of mechanism of action and therapeutic potential: A. Gescher, Crit. Rev. Oncol. Hematol. 34, 127-135 (2000). Clinical pharmacokinetics and tolerability: D. J. Propper et al., J. Clin. Oncol. 19, 1485 (2001). Clinical evaluation in diabetic macular edema: P. A. Campochiaro et al., Invest. Ophthalmol. Visual Sci. 45, 922 (2004); in acute myeloid leukemia: R. M. Stone et al., Blood 105, 54 (2005).
Properties: mp 235-247° with darkening.
Melting point: mp 235-247° with darkening
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Alkaloids/Natural Products. |