Synonym
Cgp 42700; Cgp42700; Cgp-42700
IUPAC/Chemical Name
N-((5R,6S,7S,9R)-15-benzyl-6-methoxy-5-methyl-14-oxo-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
InChi Key
ABNYYFBELSVSNV-OSODCVOKSA-N
InChi Code
InChI=1S/C42H36N4O4/c1-42-39(49-3)32(43(2)40(47)26-16-8-5-9-17-26)22-33(50-42)45-30-20-12-10-18-27(30)35-36-29(24-44(41(36)48)23-25-14-6-4-7-15-25)34-28-19-11-13-21-31(28)46(42)38(34)37(35)45/h4-21,32-33,39H,22-24H2,1-3H3/t32-,33+,39-,42+/m0/s1
SMILES Code
CO[C@H]1[C@@H](N(C(c2ccccc2)=O)C)C[C@H]3O[C@]1(n(c4c5cccc4)c6c5c(CN(C7=O)Cc8ccccc8)c7c9c6n3c%10c9cccc%10)C
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
Shelf Life
>3 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
660.77
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: Utz I, Spitaler M, Rybczynska M, Ludescher C, Hilbe W, Regenass U, Grunicke H, Hofmann J. Reversal of multidrug resistance by the staurosporine derivatives CGP 41251 and CGP 42700. Int J Cancer. 1998 Jul 3;77(1):64-9. doi: 10.1002/(sici)1097-0215(19980703)77:1<64::aid-ijc11>3.0.co;2-9. PMID: 9639395.
2: Alkan SS, Rutschmann S, Grogg D, Erb P. Effects of a new protein kinase C inhibitor CGP 41251 on T cell functions: inhibition of activation, growth, and target cell killing. Cell Immunol. 1993 Aug;150(1):137-48. doi: 10.1006/cimm.1993.1185. PMID: 8102085.
3: Chung DL, Brandt-Rauf PW, Weinstein IB, Nishimura S, Yamaizumi Z, Murphy RB, Pincus MR. Evidence that the ras oncogene-encoded p21 protein induces oocyte maturation via activation of protein kinase C. Proc Natl Acad Sci U S A. 1992 Mar 1;89(5):1993-6. doi: 10.1073/pnas.89.5.1993. PMID: 1542698; PMCID: PMC48580.
4: Conseil G, Perez-Victoria JM, Jault JM, Gamarro F, Goffeau A, Hofmann J, Di Pietro A. Protein kinase C effectors bind to multidrug ABC transporters and inhibit their activity. Biochemistry. 2001 Feb 27;40(8):2564-71. doi: 10.1021/bi002453m. PMID: 11327879.
5: Begemann M, Kashimawo SA, Heitjan DF, Schiff PB, Bruce JN, Weinstein IB. Treatment of human glioblastoma cells with the staurosporine derivative CGP 41251 inhibits CDC2 and CDK2 kinase activity and increases radiation sensitivity. Anticancer Res. 1998 Jul-Aug;18(4A):2275-82. PMID: 9703866.
6: Zimmermann A, Keller H. Effects of staurosporine, K 252a and other structurally related protein kinase inhibitors on shape and locomotion of Walker carcinosarcoma cells. Br J Cancer. 1992 Dec;66(6):1077-82. doi: 10.1038/bjc.1992.413. PMID: 1457347; PMCID: PMC1978012.
7: Loneragan K, Cheah TB, Bunn SJ, Marley PD. The role of protein kinase C in nicotinic responses of bovine chromaffin cells. Eur J Pharmacol. 1996 Sep 5;311(1):87-94. doi: 10.1016/0014-2999(96)00397-4. PMID: 8884241.
8: Grosman N. Influence of staurosporine, a more selective derivative CGP 41,251 and an inactive analogue CGP 42,700 on histamine release from isolated rat mast cells. Immunopharmacology. 1992 Jul-Aug;24(1):47-55. doi: 10.1016/0162-3109(92)90069-o. PMID: 1280632.
9: Grosman N. Influence of probes for calcium-calmodulin and protein kinase C signalling on the plasma membrane Ca2+-ATPase activity of rat synaptosomes and leukocyte membranes. Immunopharmacology. 1998 Aug;40(2):163-71. doi: 10.1016/s0162-3109(98)00042-3. PMID: 9826030.
10: Jelkmann W, Huwiler A, Fandrey J, Pfeilschifter J. Inhibition of erythropoietin production by phorbol ester is associated with down-regulation of protein kinase C-alpha isoenzyme in hepatoma cells. Biochem Biophys Res Commun. 1991 Sep 30;179(3):1441-8. doi: 10.1016/0006-291x(91)91734-t. PMID: 1656952.
