GDC-0152 (RG7419)

Alias: GDC0152; GDC 0152; GDC0152; RG-7419; RG7419; RG 7419
Cat No.:V0052 Purity: ≥98%
GDC-0152 (RG-7419) is a novel and potent antagonist of IAP (inhibitor of apoptosis) family proteins with antitumor activity.
GDC-0152 (RG7419) Chemical Structure CAS No.: 873652-48-3
Product category: IAP
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GDC-0152 (RG-7419) is a novel and potent antagonist of IAP (inhibitor of apoptosis) family proteins with antitumor activity. In cell-free assays, it inhibits IAPs with Kis of 28 nM, 14 nM, 17 nM, and 43 nM for XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3, and cIAP2-BIR3, respectively; it has a lower affinity for cIAP1-BIR2 and cIAP2-BIR2. A Phase 1 clinical trial is looking into GDC-0152 as a potential cancer treatment.

Biological Activity I Assay Protocols (From Reference)
MLXBIR3SG (Ki = 14 nM); cIAP1-BIR3 (Ki = 17 nM); XIAP-BIR3 (Ki = 28 nM); cIAP2-BIR3 (Ki = 43 nM); XIAP-BIR2 (Ki = 112 nM)
ln Vitro
GDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. GDC-0152 is demonstrated to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac as well as XIAP binding to partially processed caspase-9 using transiently transfected HEK293T cells. The endogenous association of ML-IAP and Smac is effectively also eliminated by GDC-0152 in melanoma SK-MEL28 cells. When compared to healthy human mammary epithelial cells (HMEC), GDC-0152 had no effect on HMEC but reduced cell viability in the MDA-MB-231 breast cancer cell line. It has been discovered that GDC-0152 activates caspases 3 and 7 in a dose- and time-dependent manner. In A2058 melanoma cells, GDC-0152 has been shown to cause cIAP1 to degrade rapidly. Its affinity for cIAP1 is supported by the fact that it successfully induces cIAP1 degradation at concentrations as low as 10 nM.
ln Vivo
GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays carried out using human liver microsomes.Over the range of concentrations investigated (0.1–100 μM), plasma protein binding of GDC-0152 is moderate and comparable in mice (88–91%), rats (89–91%), dogs (81–90%), monkeys (76–85%), and humans (75–83%); higher plasma protein binding is observed in rabbits (95–96%). In all tested species, GDC-0152 does not preferentially distribute to red blood cells with blood-plasma partition ratios ranging from 0.6 to 1.1. GDC-0152's pharmacokinetics are achieved with a Cmax of 53.7 μM and an AUC of 203.5 h•μM. [1]
Enzyme Assay
The IAP protein constructs are added to wells containing serial dilutions of the antagonists or the peptide AVPW, as appropriate, and the Hid-FAM probe or AVP-diPhe-FAM probe in the polarization buffer to determine the inhibitory constants (Ki) for the antagonists. After 30 minutes, samples are read. The IC50 values are calculated by fitting the data to a 4-parameter equation using software, and fluorescence polarization values are plotted as a function of antagonist concentration. Based on the IC50 values, the antagonists' Ki values are calculated.
Cell Assay
GDC-0152 is used to treat HMECs and MDA-MB-231 breast cancer cells in the recommended concentrations. The CellTiter-Glo luminescent cell viability assay is used to determine cell death 72 hours after the start of treatment.
Animal Protocol
phosphate-buffered saline; 10, 50, 100 mg/kg; Oral
Human-tumor xenograft mouse models of MDA-MB-231 breast cancer

[1]. J Med Chem . 2012 May 10;55(9):4101-13.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
Molecular Weight
Exact Mass
Elemental Analysis
C, 60.22; H, 6.87; N, 16.85; O, 9.63; S, 6.43
Related CAS #
873652-48-3;873581-21-6 (HCl);
Solid powder
InChi Key
InChi Code
Chemical Name
GDC0152; GDC 0152; GDC0152; RG-7419; RG7419; RG 7419
HS Tariff Code

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~99 mg/mL (~198.5 mM)
Water: ~3 mg/mL (~6.0 mM)
Ethanol: ~99 mg/mL (~198.5 mM)
Solubility (In Vivo)
30%Propylene glycol, 5%Tween 80, 65% D5W: 5mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0055 mL 10.0273 mL 20.0545 mL
5 mM 0.4011 mL 2.0055 mL 4.0109 mL
10 mM 0.2005 mL 1.0027 mL 2.0055 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.


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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00977067 Terminated Drug: GDC-0152 Solid Cancers Genentech, Inc. June 2007 Phase 1
Biological Data
  • GDC-0152

  • GDC-0152

  • GDC-0152

    Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.
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