Synonym
CEP11981; CEP 11981; CEP11981; BOL303213X; BOL-303213X; BOL 303213X; ESK981; ESK-981; ESK 981;
IUPAC/Chemical Name
13-isobutyl-4-methyl-10-(pyrimidin-2-ylamino)-4,7,8,13-tetrahydro-1H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-6(2H)-one
InChi Key
AEULIVPVIDOLIN-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H27N7O/c1-15(2)13-35-22-8-5-16(32-28-29-9-4-10-30-28)11-18(22)24-19-12-31-27(36)25(19)23-17(26(24)35)6-7-21-20(23)14-34(3)33-21/h4-5,8-11,14-15H,6-7,12-13H2,1-3H3,(H,31,36)(H,29,30,32)
SMILES Code
O=C1NCC2=C1C(C3=CN(C)N=C3CC4)=C4C(N5CC(C)C)=C2C6=C5C=CC(NC7=NC=CC=N7)=C6
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
>2 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
477.56
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: Pili R, Carducci M, Brown P, Hurwitz H. An open-label study to determine the maximum tolerated dose of the multitargeted tyrosine kinase inhibitor CEP-11981 in patients with advanced cancer. Invest New Drugs. 2014 Dec;32(6):1258-68. doi: 10.1007/s10637-014-0147-9. Epub 2014 Aug 26. PMID: 25152243; PMCID: PMC4226840.
2: Jian W, Levitt JM, Lerner SP, Sonpavde G. The angiopoietin-TIE2 pathway is a potential therapeutic target in urothelial carcinoma. Anticancer Res. 2014 Jul;34(7):3377-82. PMID: 24982343.
3: Eroglu Z, Stein CA, Pal SK. Targeting angiopoietin-2 signaling in cancer therapy. Expert Opin Investig Drugs. 2013 Jul;22(7):813-25. doi: 10.1517/13543784.2013.793306. Epub 2013 Apr 27. PMID: 23621441.
4: Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA. Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-m ethylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]py rrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent. J Med Chem. 2012 Jan 26;55(2):903-13. doi: 10.1021/jm201449n. Epub 2012 Jan 6. Erratum in: J Med Chem. 2012 Apr 26;55(8):4025. PMID: 22148921.
