Zandelisib(Synonyms: ME-401; PWT-143)

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Zandelisib (Synonyms: ME-401; PWT-143) 纯度: 98.79%

Zandelisib (ME-401) 是一种 PI3K 抑制剂,选择性抑制 p110δIC50 值为 3.5 nM,详细信息请参考专利文献 WO2019183226 A1 中的化合物 1。Zandelisib 具有抗肿瘤作用。

Zandelisib(Synonyms: ME-401;  PWT-143)

Zandelisib Chemical Structure

CAS No. : 1401436-95-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4440 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg ¥17000 In-stock
100 mg ¥25000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Zandelisib (ME-401) is a phosphatidylinositol 3-kinase (PI3K) inhibitor extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic[1][2].

IC50 & Target

PI3Kδ

3.5 nM (IC50)

体外研究
(In Vitro)

Zandelisib inhibits PI3Ks with IC50s of 4, 976 nM, 605 nM, 817 nM and 3.5 nM for p110α, p110β, p110γ and p110δ, respectivey[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

576.68

Formula

C31H38F2N8O

CAS 号

1401436-95-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (57.80 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7341 mL 8.6703 mL 17.3406 mL
5 mM 0.3468 mL 1.7341 mL 3.4681 mL
10 mM 0.1734 mL 0.8670 mL 1.7341 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 (4.34 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.34 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.34 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Daniel P. Gold, et al. Combination therapy. WO2019183226A1.

    [2]. David Brown, et al. (sulfinyl and sulfonyl benzimidazolyl) pyrimidines and triazines, pharmaceutical compositions thereof, and their use for treating proliferative diseases. WO2014055647A1.

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