barks of Camptotheca acuminata Decne
DMSO : 25 mg/mL (63.71 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
810.3±65.0 °C at 760 mmHg
HS Code Reference
Personal Projective Equipment
For Reference Standard and R&D, Not for Human Use Directly.
provides coniferyl ferulate(CAS#:86639-52-3) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
2018 Dec 3.
Allometry has been extensively used in the modern day drug development scenario to predict the human relevant parameters (clearance, Cl, and volume of distribution at steady state, Vss) from animal data. The applicability of allometry in the prediction of human parameters for irinotecan (CAS 97682-44-5), an important topoisomerase I inhibitor, has been retrospectively investigated. Literature pharmacokinetic data has been gathered for both irinotecan and its main metabolite, SN-38 (CAS 86639-52-3), from several animal species. The corresponding human parameters were predicted using allometry (Cl and Vss for irinotecan; Cl/F for SN-38). Although irinotecan has a complex metabolism and disposition profile, it appeared that simple allometry predicted satisfactorily the human values for Cl (1.7648W(0.669)) and Vss (3.1277W(0.9044)) for irinotecan. On the contrary, Cl/F for SN-38 was over predicted by simple allometry (53.389W(1.2773)); and the applicability of bile correction factor rendered Cl/F of SN-38 to be closer to the observed human value (8.9641W(1.3108)). The investigation suggests that prospective allometric approaches may aid in the development of future compounds in this important pharmacological and chemical class of cytotoxics.
Allometric scaling of a metabolically complex camptothecin analog: differences in scaling of irinotecan and its active metabolite, SN-38
Preeti Ahlawat 1, Nuggehally R Srinivas
Ewing sarcoma (EWS) is a tumor of the bone and soft-tissue that primarily affects adolescents and young adults. With current therapies, 70% of patients with localized disease survive, but patients with metastatic or recurrent disease have a poor outcome. We found that EWS cell lines are defective in DNA break repair and are sensitive to PARP inhibitors (PARPis). PARPi-induced cytotoxicity in EWS cells was 10- to 1,000-fold higher after administration of the DNA-damaging agents irinotecan or temozolomide. We developed an orthotopic EWS mouse model and performed pharmacokinetic and pharmacodynamic studies using 3 different PARPis that are in clinical development for pediatric cancer. Irinotecan administered on a low-dose, protracted schedule previously optimized for pediatric patients was an effective DNA-damaging agent when combined with PARPis; it was also better tolerated than combinations with temozolomide. Combining PARPis with irinotecan and temozolomide gave complete and durable responses in more than 80% of the mice.
Targeting the DNA Repair Pathway in Ewing Sarcoma
Elizabeth Stewart,1 Ross Goshorn,1 Cori Bradley,1 Lyra M. Griffiths,1 Claudia Benavente,1 Nathaniel R. Twarog,2 Gregory M. Miller,2 William Caufield,3 Burgess B. Freeman, III,3 Armita Bahrami,4 Alberto Pappo,5 Jianrong Wu,6 Amos Loh,1 asa Karlstrom,1 Chris Calabrese,7 Brittney Gordon,7 Lyudmila Tsurkan,2 M. Jason Hatfield,2 Philip M. Potter,2 Scott Snyder,2 Suresh Thiagarajan,8 Abbas Shirinifard,8 Andras Sablauer,8 Anang A. Shelat,2,* and Michael A. Dyer1,9,*
2015 May 6.