Tamanho : 10mg
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Synonyms: GDC0152
| Description | GDC-0152 is a potent inhibitor of IAPs. |
| Targets & IC50 | MLXBIR3SG:14 nM(Ki), XIAP BIR3:28 nM(Ki), XIAP BIR2:112 nM(Ki), CIAP2-BIR3:43 nM(Ki), CIAP1-BIR3:17 nM(Ki) |
| In vitro | GDC-0152 inhibits protein−protein interactions between IAP proteins and pro-apoptotic molecules. It disrupts XIAP's binding to caspase-9 and the association of ML-IAP, cIAP1, and cIAP2 with Smac in transiently transfected HEK293T cells. Similarly, in melanoma SK-MEL28 cells, GDC-0152 abolishes the natural association between ML-IAP and Smac. It decreases cell viability in the MDA-MB-231 breast cancer cell line without affecting normal human mammary epithelial cells (HMEC). Furthermore, GDC-0152 activates caspases 3 and 7 dependent on dose and time, and induces rapid degradation of cIAP1 in A2058 melanoma cells at low concentrations, aligning with its affinity for cIAP1. |
| In vivo | GDC-0152 exhibits moderate hepatic clearance as inferred from metabolic stability assays using human liver microsomes, with its plasma-protein binding being moderate yet consistent across several species, including mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) across investigated concentrations (0.1−100 μM); however, rabbits show higher plasma-protein binding rates (95−96%). Importantly, GDC-0152 does not show a preference for red blood cell distribution, as evidenced by blood-plasma partition ratios ranging from 0.6 to 1.1 across all tested species. Pharmacokinetic profiles reveal a maximum concentration (C max) of 53.7 μM and an area under the curve (AUC) of 203.5 h·μM. [1] |
| Synonyms | GDC0152 |
| Kinase Assay | Fluorescence polarization-based competition assay: Inhibition constants ( Ki ) for the antagonists are determined by addition of the IAP protein constructs to wells containing serial dilutions of the antagonists or the peptide AVPW, and the Hid-FAM probe or AVP-diPhe-FAM probe, as appropriate, in the polarization buffer. Samples are read after a 30-minute incubation. Fluorescence polarization values are plotted as a function of the antagonist concentration, and the IC50 values are obtained by fitting the data to a 4-parameter equation using software. Ki values for the antagonists are determined from the IC50 valued. |
| Cell Research | MDA-MB-231 breast carcinoma cells and HMECs are treated with the indicated concentrations of GDC-0152. Cell death is assessed using the CellTiter-Glo luminescent cell viability assay 72 h following the start of treatment.(Only for Reference) |
| Molecular Weight | 498.64 |
| Formula | C25H34N6O3S |
| Cas No. | 873652-48-3 |
| Smiles | C([C@@H](NC([C@@H](NC)C)=O)[C@@H]1CCCCC1)(=O)N2[C@H](C(NC3=C(N=NS3)C4=CC=CC=C4)=O)CCC2 |
| Relative Density. | no data available |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 92 mg/mL (184.5 mM), Sonication is recommended. Ethanol: 92 mg/mL (184.5 mM), Sonication is recommended. H2O: 3 mg/mL (6.02 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.62 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO/Ethanol
DMSO/Ethanol
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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