CLZ-8|cas:678158-55-9|西域试剂

CLZ-8,99.85%

产品编号：Bellancom-122627| CAS NO：678158-55-9| 分子式：C₂₂H₂₃N₃O₂S| 分子量：393.50

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-122627	￥1200.00	杭州北京（现货）
Bellancom-122627	￥2000.00	杭州北京（现货）
Bellancom-122627	￥4000.00	杭州北京（现货）
Bellancom-122627	￥6400.00	杭州北京（现货）
Bellancom-122627	￥10000.00	杭州北京（现货）

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CLZ-8

产品介绍

CLZ-8 (Compound 8) 是具有口服活性的 Mcl-1-PUMA 的抑制剂，K_i 值为 0.3 μM。CLZ-8 在下调 PUMA 依赖的凋亡（apoptosis）的同时还能抑制 Mcl-1 介导的癌细胞抗凋亡作用。

生物活性

CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K_i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.

体外研究

CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis.
CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA.
CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis.
CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

Cell Line:	DLD-1 cells or HUVEC cells
Concentration:	0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVECs)
Incubation Time:	48 h (DLD-1) or 24 h (HUVECs)
Result:	Significantly inhibited PUMA-dependent apoptosis with an IC₅₀ of 38.93 ± 0.91 μM. Attenuated the radiation-induced apoptosis.

Western Blot Analysis

Cell Line:	HUVEC cells
Concentration:	0.001, 0.01, 0.1 and 1 μM
Incubation Time:	2 h
Result:	Suppressed induction of PUMA after radiation, significantly decreased the level of p53. Significantly decreased the level of MCL-1 and increased the level of Bcl-XL.

体内研究
(In Vivo)

CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 week-old male BALB/c mice
Dosage:	100, 200 and 400 mg/kg
Administration:	Intragastric administration, once, 30 min prior to irradiation
Result:	Increased the survival rate of irradiated mice.

体内研究

CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 week-old male BALB/c mice
Dosage:	100, 200 and 400 mg/kg
Administration:	Intragastric administration, once, 30 min prior to irradiation
Result:	Increased the survival rate of irradiated mice.

体内研究

CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	6-8 week-old male BALB/c mice
Dosage:	100, 200 and 400 mg/kg
Administration:	Intragastric administration, once, 30 min prior to irradiation
Result:	Increased the survival rate of irradiated mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (127.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5413 mL	12.7065 mL	25.4130 mL
5 mM	0.5083 mL	2.5413 mL	5.0826 mL
10 mM	0.2541 mL	1.2706 mL	2.5413 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： 10% DMSO 90% corn oil
Solubility: ≥ 0.83 mg/mL (2.11 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (2.11 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 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。