WM-1119|cas:2055397-28-7|西域试剂

WM-1119,99.83%

产品编号：Bellancom-102058| CAS NO：2055397-28-7| 分子式：C₁₈H₁₃F₂N₃O₃S| 分子量：389.38

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货号	价格	库存与货期
Bellancom-102058	￥1100.00	杭州北京（现货）
Bellancom-102058	￥1900.00	杭州北京（现货）
Bellancom-102058	￥3600.00	杭州北京（现货）
Bellancom-102058	￥6500.00	杭州北京（现货）
Bellancom-102058	￥10500.00	杭州北京（现货）

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WM-1119

产品介绍

WM-1119 是强效的、选择性 KAT6A 抑制剂，淋巴瘤细胞中测得对 KAT6A的 IC₅₀ 值为 0.25 μM，对 KAT6A，KAT5，KAT7 的结合 K_D 值分别为 2 nM，2.2 μM，0.5 μM。

生物活性

WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC₅₀ of 0.25 μM for KAT6A in lymphoma cells, the binding K_D values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.

体外研究

WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. WM-1119 is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively, and so shows greater specificity for KAT6A than does WM-8014. Treatment of MEFs with WM-1119 results in cell cycle arrest in G1 and a senescence phenotype similar to that seen upon treatment with WM-8014. Notably, the activity of WM-1119 in this cell-based assay is an order of magnitude greater than WM-8014 and WM-1119 is able to induce cell cycle arrest at 1 μM. Treatment with WM-1119 inhibits the proliferation of the EMRK1184 lymphoma cells in vitro, WM-1119 (IC₅₀=0.25 μM) is ninefold more active than WM-8014 (IC₅₀=2.3 μM), as expected on the basis of reduced protein binding.

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

体内研究

By day 14, the cohorts that are treated four times per day with WM-1119 have arrested tumour growth, with the exception of one mouse that does not respond. Spleen weights in the WM-1119-treatment group (treated four times per day) are substantially lower than spleen weights in the vehicle-treated group. Treatment with WM-1119 three times per day leads to a significant reduction in tumour burden and spleen weight, but is not as effective as treatment four times per day. WM-1119 is well-tolerated; mice show no generalized ill effects and weight loss is not observed. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day).

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (321.02 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5682 mL	12.8409 mL	25.6819 mL
5 mM	0.5136 mL	2.5682 mL	5.1364 mL
10 mM	0.2568 mL	1.2841 mL	2.5682 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.42 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.34 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。