GDC 0152.
GDC-0152
CAS: 873652-48-3
Molecular Formula: C25H34N6O3S
GDC 0152. - Names and Identifiers
GDC 0152. - Physico-chemical Properties
| Molecular Formula | C25H34N6O3S |
| Molar Mass | 498.64 |
| Melting Point | 175-177oC |
| Solubility | DMSO (Slightly) |
| Appearance | Solid |
| Color | White |
| Storage Condition | -20°C Freezer |
| In vitro study | GDC-0152 blocks protein-protein interactions in which IAP proteins and pro-apoptotic molecules are involved. GDC-0152 transient transfection of HEK293T cells appeared to disturb caspase-9 of XIAP binding moiety treatment and ML-IAP,CIAP1,cIAP2 and Smac protein binding. In melanoma SK-MEL28 cells, GDC-0152 effectively inhibited ML-IAP of endogenous binding to the Smac protein. Of the MDA-MB-231 breast cancer cell lines, GDC-0152 resulted in a decrease in cell viability without an effect on normal human mammary epithelial cells (HMEC). GDC-0152 activates caspases 3 and 7 in a dose and time dependent manner. In A2058 melanoma cells, GDC-0152 induced rapid degradation of ciap1. At concentrations as low as 10 nM, it efficiently induced CIAP1 degradation, consistent with its affinity for ciap1. GDC-0152 blocks protein-protein interactions in which IAP proteins and pro-apoptotic molecules are involved. GDC-0152 transient transfection of HEK293T cells appeared to disturb caspase-9 of XIAP binding moiety treatment and ML-IAP,CIAP1,cIAP2 and Smac protein binding. In melanoma SK-MEL28 cells, GDC-0152 effectively inhibited ML-IAP of endogenous binding to the Smac protein. Of the MDA-MB-231 breast cancer cell lines, GDC-0152 resulted in a decrease in cell viability without an effect on normal human mammary epithelial cells (HMEC). GDC-0152 activates caspases 3 and 7 in a dose and time dependent manner. In A2058 melanoma cells, GDC-0152 induced rapid degradation of ciap1. At concentrations as low as 10 nM, it efficiently induced CIAP1 degradation, consistent with its affinity for ciap1. |
| In vivo study | GDC-0152 had predicted moderate liver clearance based on metabolic stability analysis using human liver microsomes. The binding of plasma proteins to GDC-0152 was moderate, with binding rates in mice (88-0.1), rats (89-100) at concentrations of (91%-91% μm), there was no difference in dogs (81-90%), monkeys (76-85%) and humans (75-83%); Higher in rabbits (95-96%). The blood plasma distribution ratios ranged from 0.6 to 1.1 in all species tested and were not preferentially distributed among red blood cells GDC-0152. The pharmacokinetics GDC-0152 was a Cmax of 53.7 μm and an AUC of 203.5 h-μm. GDC-0152 had a moderate hepatic clearance effect based on prediction of metabolic stability analysis using human liver microsomes. The binding of plasma proteins to GDC-0152 was moderate, with binding rates in mice (88-0.1), rats (89-100) at concentrations of (91%-91% μm), there was no difference in dogs (81-90%), monkeys (76-85%) and humans (75-83%); Higher in rabbits (95-96%). The blood plasma distribution ratios ranged from 0.6 to 1.1 in all species tested and were not preferentially distributed among red blood cells GDC-0152. The pharmacokinetics GDC-0152 was C max of 53.7 μm and AUC of 203.5 h-μm. |
GDC 0152. - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.005 ml | 10.027 ml | 20.055 ml |
| 5 mM | 0.401 ml | 2.005 ml | 4.011 ml |
| 10 mM | 0.201 ml | 1.003 ml | 2.005 ml |
| 5 mM | 0.04 ml | 0.201 ml | 0.401 ml |
Last Update：2024-01-02 23:10:35
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