CCT018159 - CAS:171009-07-7

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CCT018159

目录号 : KCM11947 CAS No. : 171009-07-7 纯度 : ≥98%

Data Sheet 产品使用指南

The heat shock protein 90 (Hsp90) is a molecular chaperone that activates and maintains the biological functioning of several client proteins, many of which are associated with oncogenic signaling pathways. Its activity is driven by ATP and regulated by co-chaperones such as Hsp72. CCT018159 is a 3,4-diaryl pyrazoloresorcinol compound that inhibits the ATPase activity of Hsp90 with IC values of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. At concentrations up to 100 µM, CCT018159 does not inhibit human Hsp72 ATPase or topoisomerase II, yet at 50 µM CCT018159 inhibits 13 out of a panel of 20 commonly studied kinases. In human tumor xenografts, such as SKMEL 28 melanoma cells, CCT018159 induces Hsp72 expression and dc-Raf, ERBB2, and Cdk4.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

CCT018159 is an ATP-competitive HSP90β inhibitor, with an IC50 of 3.2 μM against human HSP90β ATPase and 6.6 μM against yeast HSP90β ATPase. CCT018159 induces cell cycle arrest and apoptosis in tumor cells, and inhibits invasion and angiogenesis. CCT018159 is applicable to cancer-related research.

体外研究

CCT018159 can inhibit the growth of human cancer cell lines, with an average GI50 of 5.3 μM. Its activity against HUVECs (GI50: 0.87 μM) is stronger than most cancer cell lines .
CCT018159 (24 h) can induce characteristic molecular markers of HSP90 inhibition, including upregulation of HSP72 in human cancer cells, depletion of substrate proteins (C-RAF, CDK4, ERBB2, mutant B-RAF), and decreased phosphorylation levels of ERK1/2. It can also regulate angiogenesis related substrate proteins in HUVECs.
CCT018159 (41 μM; 16-72 h) can induce cell cycle arrest and apoptosis in SKMEL 5 melanoma cells.
CCT018159 (0-4.4 μM; 24-48 h) can inhibit key functions of endothelial cells and invasion related functions of tumor cells.
CCT018159 (0.1-50 μM) can dose dependently reduce the viability of NCI-H295R cells, with an EC50 of 11.5 μM.

Cell Cycle Analysis

Cell Line:	SKMEL 5
Concentration:	41 μmol/L
Incubation Time:	16, 24, 48, 72 hours
Result:	Caused marked accumulation of SKMEL 5 melanoma cells in the G1 phase by 16 h, with cells arrested in the initial G1 or subsequent G1 phase through 72 h.

分子式

C₂₀H₂₀N₂O₄

分子量

352.38

CAS号

171009-07-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (283.78 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8378 mL	14.1892 mL	28.3785 mL
5 mM	0.5676 mL	2.8378 mL	5.6757 mL
10 mM	0.2838 mL	1.4189 mL	2.8378 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 (protect from light))。-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 → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.09 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。
2.

请依序添加每种溶剂：10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.09 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。