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GDC-0152

Chemical Structure : GDC-0152

CAS No.: 873652-48-3

GDC-0152 (GDC0152)

Catalog No.: PC-25916Not For Human Use, Lab Use Only.

GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins, binds to XIAP BIR3 domain, BIR domain of ML-IAP, and BIR3 domains of cIAP1 and cIAP2 with Ki of 28, 14, 17, and 43 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins, binds to XIAP BIR3 domain, BIR domain of ML-IAP, and BIR3 domains of cIAP1 and cIAP2 with Ki of 28, 14, 17, and 43 nM, respectively.
GDC-0152 promotes degradation of cIAP1, induces activation of caspase-3/7, and lead to decreased viability of breast cancer cells without affecting normal mammary epithelial cells.
GDC-0152 (10-100 mg/kg) inhibits tumor growth when dosed orally in the MDA-MB-231 breast cancer xenograft model.

Physicochemical Properties

M.Wt 498.65
Formula C25H34N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-((S)-2-Cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)-N-(4-phenyl-1,2,3-thiadiazol-5-yl)pyrrolidine-2-carboxamide

References

1. Flygare JA, et al. J Med Chem. 2012 May 10;55(9):4101-13.

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