XL888

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Chemical Structure| 1149705-71-4 同义名 : -
CAS号 : 1149705-71-4
货号 : A399992
分子式 : C29H37N5O3
纯度 : 99%+
分子量 : 503.64
MDL号 : MFCD22124888
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.93mL

1.99mL

0.99mL

19.86mL

3.97mL

1.99mL
参考文献

[1]22(17):5396-404.

[2]6(3):e17692.