| CAS NO: | 518303-20-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 468.34 |
|---|---|
| Formula | C18H14BrNO5S2 |
| CAS No. | 518303-20-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 93 mg/mL (198.6 mM) |
| Water: <1 mg/mL (slightly soluble or insoluble) | |
| Ethanol: Not available | |
| Solubility (In vivo) | 5% DMSO+30% PEG 300+dd H2O: 6 mg/mL |
| General | In a BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg i.v.) exhibits single-agent antitumor activity without any damage normal tissues |
|---|---|
| Animal model | Female BALB/c or CB17 SCID/SCID mice bearing SW480, C33A, PC3, and 4T1 cells. |
| Formulation | Obatoclax (tartrate salt) is formulated in 9.6% PEG300, 0.4% polysorbate 20, and 5% dextrose; while for the 4T1 tumor model, Obatoclax is formulated in 9.48% PEG, 0.38% polysorbate 20. |
| Dosages | 0.0313, 0.25, 0.5 and 2 mg/kg |
| Administration | Intravenously (tail vein) once a day |
| References | [1] Abulwerdi F, et al. Mol Cancer Ther. 2014, 13(3), 565-575. |
 UMI77 disrupts the Mcl-1/Bak complex. Panc-1 (A) and BxPC-3 (B) cells were treated with the indicated concentrations of UMI77 for 48 hours and then prepared for immunoprecipitation and immunoblotting. Mcl-1 was immunoprecipitated from cell lysates and the levels of Bak interacting with Mcl-1 were detected by immunoblotting for Bak. Translational oncology 8(1):47-54, 2015 |  Downregulation of Mcl-1 by siRNA in BxPC-3 cells blocks growth inhibition and apoptosis induced by 2 (UMI-77). Mol Cancer Ther. 2014 Mar;13(3):565-75 |  Inhibition of Mcl-1 by UMI77 does not radiosensitize normal cells. CCL-241 normal small intestinal cells were treated with UMI77 (1-3μM) as illustrated (Figure 3A) and radiosensitization was assessed by clonogenic survival. Translational oncology 8(1):47-54, 2015 |
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