GDC-0152 (RG7419)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $980 | Check With Us |
| 500mg | $1420 | Check With Us |
| 1g | $2130 | Check With Us |
: Cat #: V0052 CAS #: 873652-48-3 Purity ≥ 98%
Description: GDC-0152 (RG-7419) is a novel and potent antagonist of IAP (inhibitor of apoptosis) family proteins with antitumor activity.
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| Molecular Weight (MW) | 498.64 |
|---|---|
| Molecular Formula | C25H34N6O3S |
| CAS No. | 873652-48-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 99 mg/mL (198.5 mM)r |
| Water: 3 mg/mL (6.0 mM)r | |
| Ethanol: 99 mg/mL (198.5 mM) | |
| Solubility In Vivo | 30% Propylene glycol, 5% Tween 80, 65% D5W: 5mg/mL |
| SMILES Code | O=C([C@H]1N(C([C@H](C2CCCCC2)NC([C@@H](NC)C)=O)=O)CCC1)NC3=C(C4=CC=CC=C4)N=NS3 |
| Synonyms | RG 7419; RG-7419; RG7419; GDC0152; GDC0152; GDC 0152; |
| Protocol | In Vitro | GDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac. In melanoma SK-MEL28 cells, the endogenous association of ML-IAP and Smac is also effectively abolished by GDC-0152. GDC-0152 leads to a decrease in cell viability in the MDA-MB-231 breast cancer cell line, while having no effect on normal human mammary epithelial cells (HMEC). GDC-0152 is found to activate caspases 3 and 7 in a dose- and time-dependent manner. GDC-0152 is shown to induce rapid degradation of cIAP1 in A2058 melanoma cells. It effectively induces degradation of cIAP1 at concentrations as low as 10 nM, consistent with its affinity for cIAP1. |
|---|---|---|
| In Vivo | GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma−protein binding of GDC-0152 is moderate and comparable among mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) over the range of concentrations investigated (0.1−100 μM); higher plasma−protein binding is observed in rabbits (95−96%). GDC-0152 does not preferentially distribute to red blood cells with blood−plasma partition ratios ranging from 0.6 to 1.1 in all species tested. The pharmacokinetics for GDC-0152 is achieved with a C max of 53.7 μM and AUC of 203.5 h·μM. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0055 mL | 10.0273 mL | 20.0545 mL | 40.1091 mL |
| 5mM | 0.4011 mL | 2.0055 mL | 4.0109 mL | 8.0218 mL |
| 10mM | 0.2005 mL | 1.0027 mL | 2.0055 mL | 4.0109 mL |
| 20mM | 0.1003 mL | 0.5014 mL | 1.0027 mL | 2.0055 mL |
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Method for preparing in vivo formulation:
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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