product name Birinapant
References: Breast Cancer Res Treat. 2013 Jan;137(2):359-71.
806.94
Formula
C42H56F2N8O6
CAS No.
1260251-31-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (123.9 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 55 mg/mL (68.1 mM)
Solubility (In vivo)
15% Captisol: 15mg/mL
Chemical Name
(2S,2S)-N,N-((2S,2S)-((3S,3S,5R,5R)-5,5-((6,6-difluoro-1H,1H-[2,2-biindole]-3,3-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-2,1-diyl))bis(2-(methylamino)propanamide)
other peoduct :
| Birinapant binds with XIAP and cIAP1 with Kd of 45 and <1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. Birinapant in combination with TNF-α(1 ng/mL) inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively. | |
|---|---|
| In Vivo | Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. |
| Animal model | Human melanoma xenografts 451Lu |
| Formulation & Dosage | 12.5% Captisol in distilled water; 30 mg/kg; i.p. 3 times per week |
| References | [1] Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794. |
