CUDC-427
CUDC-427 Basic information
- Product Name:
- CUDC-427
- Synonyms:
-
- CUDC-427
- GDC 0917
- GDC0917
- GDC-0917
- L-Prolinamide, N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-N-[2-(2-oxazolyl)-4-phenyl-5-thiazolyl]-
- CUDC-427 (GDC-0917)
- GDC-0917 (CUDC-427)
- CUDC 427,CUDC427
- CAS:
- 1446182-94-0
- MF:
- C29H36N6O4S
- MW:
- 564.7
- Mol File:
- 1446182-94-0.mol
CUDC-427 Chemical Properties
- Density
- 1.281±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 61 mg/mL (108.02 mM)
- form
- Solid
- pka
- 11.78±0.20(Predicted)
- color
- Light yellow to yellow
CUDC-427 Usage And Synthesis
Uses
CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.
in vivo
GDC-0917 (0.08-16.3 mg/kg) exhibits antitumor activity in a dose dependent manner in the MDA-MB-231-X1.1 Breast Cancer Xenograft, and GDC-0917 is well tolerated, with all dose groups experiencing a <11% decrease in mean body weight. GDC-0917 has low to moderate clearance in the mouse (12.0 mL/min/kg), rat (27.0 mL/min/kg), and dog (15.3 mL/min/kg), and high clearance in the monkey (67.6 mL/min/kg). Oral bioavailability is lowest in monkeys compared with other species[1].
References
[1] Wong H, et al. Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist. Drug Metab Dispos. 2013 Dec;41(12):2104-13. DOI:10.1124/dmd.113.053926
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