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抑制剂/激活剂

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凋亡与自噬

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CB-5083

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。

货号：
TK0270
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1542705-92-9
生物活性	CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM。
分子式	C24H23N5O2
分子量	413.47
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 100 mg/mL (241.86 mM; Need ultrasonic)
体内研究	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 (T1/2=2.56 h), moderate oral bioavailability (mouse 41%) and Cmax (mouse 7.95 μM) following oral administration (25 mg/kg) in female nude mice. CB-5083 exhibits terminal elimination half-life (T1/2=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 T1/2 in a mouse liver microsomal stability study and a 172 min T1/2 in a hepatocyte stability study.
体外研究	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.
文献	•Cell. 2020 Dec 10;183(6):1714-1731.e10. •Sci Adv. 2021 May 14;7(20):eabg2099. •Leukemia. 2019 Jul;33(7):1675-1686. •Cell Rep. 2021 May 25;35(8):109153. •Mol Ther Oncolytics. 2020 Jun 23;18:215-225. •J Biol Chem. 2019 Dec 27;294(52):20084-20096. •J Virol. 2021 May 5;JVI.00531-21. •J Virol. 2021 Feb 3;JVI.02399-20. •Biochem Biophys Res Commun. 2021 Mar 3;549:150-156. •PLoS One. 2021 Aug 24;16(8):e0256640.
纯度及产品资料	98%

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