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CAS No.: 1149705-71-4

XL888 Catalog No. CSN16304

Synonyms: XL888

XL888 is a specific and ATP-competitive Hsp90 inhibitor with IC50 of 24 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HSP90

IC50:24nM
描述Heat shock protein 90 (HSP90) is a molecular chaperone responsible for maintaining proteostasis in cells. XL888 is a HSP90 inhibitor with an IC50 value of 24 nM. In NCI-N87 cells, XL888 resulted in HER2 degradation with an IC50 value of 56 nM. In NCI-N87, BT-474, and MDA-MB-453 cell lines overexpressing HER2, the proliferation IC50 values were 21.8, 0.1, and 16.0 nM, respectively. In Colo-205, SK-MEL-28 cell lines with B-Raf mutation, the proliferation IC50 values were 11.6 and 0.3 nM, respectively^[3]. When WM-266-4 cells were treated with 370 nM XL888 for 24h, the number of cells at S phase was decreased and the 4N DNA content in cells were accumulated compared to DMSO-treated cells. The incubation of MCF-7 cells with XL888 (35 – 556 nM) for 24h resulted in a significant reduction in S phase accompanied with an increase in M (+/-G2). After the treatment with 123 nM XL888 for 18h, CHL-1 cells showed M phase arrest with highly organized chromosomes in a linear, metaphase-like configuration compared to DMSO-treated group. In two M-class lines (CHL-1 and EBC-1), XL888 at 14 – 1670 nM dose-dependently decreased PLK1 level after 4 – 12h post treatment^[4]. In NCI-N87 xenograft mouse model, XL888 treatment at 60 mpk (once per day) led to 100% tumor growth inhibition 27d post implantation, whereas dosing at 100 mpk (once per day for 3 days, every 7 days) exceeded 100% tumor growth inhibition and demonstrated 21% tumor regression^[3].
作用机制XL888 inhibits HSP90 in an ATP-competitive mode^[3].
动物研究
剂量
Mice: 100 mg/kg^[2] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 100 mg/kg^[2] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01657591	Melanoma	Phase 1	Active, not recruiting	June 2019	United States, Florida ... more >> H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 Collapse <<
NCT00796484	Cancer	Phase 1	Terminated(Sponsor decision)	-	United States, Pennsylvania ... more >> Hospital of the University of Pennsylvania Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas South Texas Accelerated Research Therapeutics San Antonio, Texas, United States, 78229 Collapse <<
NCT02721459	Melanoma Skin... more >> Cancer Collapse <<	Phase 1	Active, not recruiting	December 2021	United States, Florida ... more >> H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9856 mL
- 9.9278 mL
- 19.8556 mL
- 5 mM
- 0.3971 mL
- 1.9856 mL
- 3.9711 mL
- 10 mM
- 0.1986 mL
- 0.9928 mL
- 1.9856 mL

技术信息

CAS号

1149705-71-4

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H37N5O3

运输

蓝冰

分子量

503.64

别名

XL888

溶解度

DMSO	240.0 mg/mL (476.5 mM)
Water	insoluble

动物实验配方

30% PEG400+0.5% Tween80+5% propylene glycol+water

30 mg/mL

suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01657591	Melanoma	Phase 1	Active, not recruiting	June 2019	United States, Florida ... more >> H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 Collapse <<
NCT00796484	Cancer	Phase 1	Terminated(Sponsor decision)	-	United States, Pennsylvania ... more >> Hospital of the University of Pennsylvania Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas South Texas Accelerated Research Therapeutics San Antonio, Texas, United States, 78229 Collapse <<
NCT02721459	Melanoma Skin... more >> Cancer Collapse <<	Phase 1	Active, not recruiting	December 2021	United States, Florida ... more >> H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 Collapse <<
NCT03095781	Adenocarcinoma of the Gastroes... more >>ophageal Junction Colorectal Adenocarcinoma Metastatic Pancreatic Adenocarcinoma Non-Resectable Cholangiocarcinoma Non-Resectable Hepatocellular Carcinoma Recurrent Cholangiocarcinoma Recurrent Colorectal Carcinoma Recurrent Gastric Carcinoma Recurrent Hepatocellular Carcinoma Recurrent Pancreatic Carcinoma Recurrent Small Intestinal Carcinoma Small Intestinal Adenocarcinoma Stage III Colorectal Cancer Stage III Gastric Cancer Stage III Hepatocellular Carcinoma Stage III Pancreatic Cancer Stage III Small Intestinal Cancer Stage IIIA Colorectal Cancer Stage IIIA Gastric Cancer Stage IIIA Hepatocellular Carcinoma Stage IIIA Small Intestinal Cancer Stage IIIB Colorectal Cancer Stage IIIB Gastric Cancer Stage IIIB Hepatocellular Carcinoma Stage IIIB Small Intestinal Cancer Stage IIIC Gastric Cancer Stage IV Colorectal Cancer Stage IV Gastric Cancer Stage IV Hepatocellular Carcinoma Stage IV Pancreatic Cancer Stage IV Small Intestinal Cancer Stage IVA Colorectal Cancer Stage IVA Hepatocellular Carcinoma Stage IVA Pancreatic Cancer Stage IVB Colorectal Cancer Stage IVB Hepatocellular Carcinoma Stage IVB Pancreatic Cancer Unresectable Pancreatic Carcinoma Unresectable Small Intestinal Carcinoma Collapse <<	Phase 1	Recruiting	June 2023	United States, Georgia ... more >> Emory University Hospital Midtown Recruiting Atlanta, Georgia, United States, 30308 Contact: Shabnam Montazeri 404-686-0242 shabnam.montazeri@emory.edu Contact: Swathi Chinaranagari 404-686-0239 swathi.chinaranagari@emory.edu Emory University/Winship Cancer Institute Recruiting Atlanta, Georgia, United States, 30322 Contact: Audrey Atkins 404-778-4389 audrey.m.adkins@emory.edu Contact: Meredith Renfroe 404-778-2670 marenfr@emory.edu Emory Saint Joseph's Hospital Recruiting Atlanta, Georgia, United States, 30342 Contact: Alicia Escobar 678-843-7029 alicia.m.escobar@emory.edu Contact: Krystal Reese 678-843-5911 krystal.reese@emory.edu Collapse <<

XL888 Catalog No. CSN16304

靶点选择性

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