Molecular Weight(MW): 468.34
UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
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|Description||UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.|
UMI-77 effectively disrupts the interactions between BL-Noxa and cellular Mcl-1, as well as Mcl-1/Bax protein–protein interactions.  UMI-77 inhibits growth of pancreatic cancer cells with IC50 of 3.4, 4.4, 12.5, 16.1, and 5.5 μM for BxPC-3, Panc-1, MiaPaCa-2, AsPC-1 and Capan-2 cells, respectively. UMI-77 induced apoptosis in pancreatic cancer through activation of the intrinsic apoptotic pathway and/or Bax conformational change. 
|In vivo||In a BxPC-3 xenograft mouse model, UMI-77 (60 mg/kg i.v.) exhibits single-agent antitumor activity without any damage normal tissues. |
Fluorescence polarization (FP)-based binding assays:Based on the Kd values, the concentrations of the proteins used in the competitive binding experiments are 90 nM for Mcl-1, 40 nM for Bcl-w, 50 nM for Bcl-xL, 60 nM for Bcl-2, and 4 nM for A1/Bfl-1. The fluorescent probes, Flu-BID and FAM-BID are fixed at 2 nM for all assays except for A1/Bfl-1 where FAMBID is used at 1 nM. 5 μL of the tested compound in DMSO and 120 μL of protein/probe complex in the assay buffer (100 mM potassium phosphate, pH 7.5; 100 μg/ml bovine gamma globulin; 0.02% sodium azide) are added to assay plates (Microfluor 2Black), incubated at room temperature for 3 h and the polarization values (mP) are measured at an excitation wavelength at 485 nm and an emission wavelength at 530 nm using the plate reader Synergy H1Hybrid. IC50 values are determined by nonlinear regression fitting of the competition curves.
|In vitro||DMSO||93 mg/mL (198.57 mM)|
|Ethanol||93 mg/mL warmed (198.57 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+30% PEG 300+dd H2O
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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