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CB-5083

CAS No. : 1542705-92-9

MCE 站：CB-5083

产品活性：CB-5083 是一种首创的，有效的，具有口服活性的，选择性 p97 AAA ATPase/VCP 抑制剂。CB-5083 抑制 p97 AAA ATP 酶结构域 D2，IC₅₀ 为 11 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：p97

In Vitro: CB-5083 shows cell killing potency with IC₅₀s of 0.68, 0.68, 1.03, and 0.49 μM for lung carcinoma A549 CTG, A549 K48, A549 CHOP, and A549 p62, respectively.

In Vivo: CB-5083 (75 mg/kg; oral administration; qd; for 2 weeks) shows antitumor activity in an HCT 116 tumor xenograft model.
CB-5083 exhibits terminal elimination half-life (T_1/2=2.56 h), moderate oral bioavailability (mouse 41%) and C_max (mouse 7.95 μM) following oral administration (25 mg/kg) in female nude mice.
CB-5083 exhibits terminal elimination half-life (T_1/2=2.83 h) due to high plasma clearance (5.9 mL/min/kg respectively) combined with large volumes of distribution (418 mL/kg respectively) following intravenous administration (3.0 mg/kg) in female nude mice.
CB-5083 has good metabolic stability with a 102 min T_1/2 in a mouse liver microsomal stability study and a 172 min T_1/2 in a hepatocyte stability study.

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