Cat. No. Name Size Price Add Cart
KI2345GDC-015210 mg$432
GDC-0152100 mg$2672

Chemical Characteristic

Product NameGDC-0152
SynonymsN/A
CAS No.873652-48-3
Molecular Weight 498.64
FormulaC25H34N6O3S
Chemical Name(S)-1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)-N-(4-phenyl-1,2,3-thiadiazol-5-yl)pyrrolidine-2-carboxamide ??
SmilesC(=O)(C1N(CCC1)C(=O)C(NC(=O)[C@@H](NC)C)C1CCCCC1)Nc1snnc1c1ccccc1
Chemical Structure

Biological activities

GDC-0152 is a potent antagonist of cellular IAP1/2 (cIAP1/2), melanoma IAP (ML-IAP), and X chromosome-linked IAP (XIAP). GDC-0152 binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with Ki values of 28, 14, 17 and 43 nM, respectively. GDC-0152 promotes degradation of cIAP1, induces the activation of caspase-3/7, and leads to decreased viability of breast cancer cells without affecting normal mammary epithelial cells. GDC-0152 inhibits tumor growth in the MDA-MB-231 breast cancer mouse xenograft model.[1]

References

[1] Flygare JA, et al. Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152). J Med Chem. 2012, 55(9): 4101-4113.

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