| CAS NO: | 1260251-31-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 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 |
| Synonym | TL32711; TL-32711; TL 32711; SMAC mimetic; Birinapant |
| Chemical Name | (2S,2'S)-N,N'-((2S,2'S)-((3S,3'S,5R,5'R)-5,5'-((6,6'-difluoro-1H,1'H-[2,2'-biindole]-3,3'-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-2,1-diyl))bis(2-(methylamino)propanamide) |
| In Vitro | 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. |
|
|  Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794. |  Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794. |
m.cnreagent.com
