CUDC-427

Research use only, not for human use.

CUDC-427 (GDC-0917) is an orally bioactive and pan antagonist of inhibitor of apoptosis proteins(IAPs). CUDC-427 can be used in research on cancers.

CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.

GDC-0917 (0.1 nM-10 μM) induces reduction of cIAP1 levels in PBMCs in a concentration-dependent manner showing greater than 80% inhibition at concentrations greater than 0.1 μM (56.5 ng/mL).

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.

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Apoptosis

IAP

IAP

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1446182-94-0

564.7

C29H36N6O4S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (88.54 mM; Ultrasonic )

CN[C@@H](C)C(=O)N[C@@H](C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)Nc1sc(nc1-c1ccccc1)-c1ncco1

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(-20℃)

With Ice Pack

≥ 2 years