CB-5083
目录号 : KM3823 CAS No. : 1542705-92-9 纯度 : 98%

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。

规格 价格 是否有货 数量
2mg
In-stock
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

KKL Med 的所有产品和服务仅用于科学研究,不能被用于人体,兽医,我们也不向个人提供产品和服务。
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。

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.

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.

Animal Model: Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon
Dosage: 75 mg/kg
Administration: Administered orally using every day (qd) dosing, for 2 weeks.
Result: Showed more profound antitumor activity.
分子式
C24H23N5O2
分子量
413.47
CAS号
1542705-92-9
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (241.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 10 mg/mL (24.19 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.05 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.05 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.05 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
在线客服
咨询热线
400-881-9290
关注微信公众号