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CB-5083 is a first-in-class, potent and selective, orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM.
CB-5083 (75 mg/kg; oral administration; qd; for 2 weeks) shows antitumor activity in an HCT 116 tumor xenograft model.
Molecular Weight | 413.47 |
Formula | C24H23N5O2 |
CAS Number | 1542705-92-9 |
Solubility (25°C) | DMSO 90 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Related p97 Products |
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CB-5339
CB-5339 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07). |
DBeQ
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 μM. |
NMS-873
NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with an IC50 value of 30 nM. |
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