Synonym
CGP52421; CGP-52421; CGP 52421.
IUPAC/Chemical Name
N-((5S,7S,8S,10R)-15-hydroxy-8-methoxy-10-methyl-17-oxo-6,7,8,9,10,15,16,17-octahydro-5H-18-oxa-4b,10a,16-triaza-5,10-methanodibenzo[b,h]cyclodeca[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
InChi Key
WMQSFYBLPAXEDG-VPROBEFOSA-N
InChi Code
InChI=1S/C36H32N4O5/c1-36-18-25(44-3)24(38(2)35(43)19-11-5-4-6-12-19)17-26(45-36)39-22-15-9-7-13-20(22)27-29-30(34(42)37-33(29)41)28-21-14-8-10-16-23(21)40(36)32(28)31(27)39/h4-16,24-26,34,42H,17-18H2,1-3H3,(H,37,41)/t24-,25-,26-,34?,36+/m0/s1
SMILES Code
O=C(N([C@H]1C[C@@](O2)([H])N3C4=CC=CC=C4C5=C3C6=C(C7=CC=CC=C7N6[C@@]2(C)C[C@@H]1OC)C(C(O)N8)=C5C8=O)C)C9=CC=CC=C9
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>5 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
600.66
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Yin OQ, Wang Y, Schran H. A mechanism-based population pharmacokinetic model for characterizing time-dependent pharmacokinetics of midostaurin and its metabolites in human subjects. Clin Pharmacokinet. 2008;47(12):807-16. doi: 10.2165/0003088-200847120-00005. PubMed PMID: 19026036.
2: Wang Y, Yin OQ, Graf P, Kisicki JC, Schran H. Dose- and time-dependent pharmacokinetics of midostaurin in patients with diabetes mellitus. J Clin Pharmacol. 2008 Jun;48(6):763-75. doi: 10.1177/0091270008318006. PubMed PMID: 18508951.
3: Illmer T, Thiede HM, Thiede C, Bornhäuser M, Schaich M, Schleyer E, Ehninger G. A highly sensitive method for the detection of PKC412 (CGP41251) and its metabolites by high-performance liquid chromatography. J Pharmacol Toxicol Methods. 2007 Jul-Aug;56(1):23-7. Epub 2007 Feb 23. PubMed PMID: 17395497.
4: Levis M, Brown P, Smith BD, Stine A, Pham R, Stone R, Deangelo D, Galinsky I, Giles F, Estey E, Kantarjian H, Cohen P, Wang Y, Roesel J, Karp JE, Small D. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors. Blood. 2006 Nov 15;108(10):3477-83. Epub 2006 Jul 20. PubMed PMID: 16857987; PubMed Central PMCID: PMC1895426.