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- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1542705-92-9
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1210.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥440.0 |
| 规格： | 5 mg | 产品价格： | ￥1100.0 |
| 规格： | 10 mg | 产品价格： | ￥1700.0 |
| 规格： | 25 mg | 产品价格： | ￥3800.0 |
| 规格： | 50 mg | 产品价格： | ￥6100.0 |
| 规格： | 100 mg | 产品价格： | ￥9800.0 |
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CB-5083
CAS No. : 1542705-92-9
MCE 国际站：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 (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.
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The Nitroreductase/CB1954 Enzyme-Prodrug System
The prodrug CB1954 (5-[aziridin-1-yl]-2,4-dinitrobenzamide) is a weak monofunctional alkylating agent originally synthesized at the Chester Beatty Laboratories in the late 1960s (1 ). The antitumor activity of CB1954 was determined
snip-SNP mapping with CB4856 polymorphisms
snip-SNP mapping with CB4856 polymorphisms Materials: Worm Lysis Buffer PCR reagents PCR primers flanking a SNP 2X restriction mix with the appropriate enzyme Procedure:
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