CXD101

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CXD101  纯度: 99.71%

CXD101 是一种有效的,选择性的,具有口服活性的 I 类 HDAC 抑制剂,对 HDAC1HDAC2HDAC3IC50 分别为 63 nM,570 nM 和 550 nM。CXD101 对 II 类 HDAC 没有活性,并具有抗肿瘤活性。

CXD101

CXD101 Chemical Structure

CAS No. : 934828-12-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1509 In-stock
1 mg ¥700 In-stock
5 mg ¥1700 In-stock
10 mg ¥2500 In-stock
50 mg ¥7600 In-stock
100 mg ¥12000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CXD101 相关产品

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生物活性

CXD101 is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. CXD101 has no activity against HDAC class II. CXD101 has antitumor activity[1][2].

IC50 & Target[1]

HDAC1

63 nM (IC50)

HDAC3

550 nM (IC50)

HDAC2

570 nM (IC50)

体外研究
(In Vitro)

CXD101 has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC50s ranged from 0.2 to 15 μM[2].

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.

体内研究
(In Vivo)

CXD101 substantially reduces tumor size in murine xenograft lung (A549a) and colon (HT29) models at a dose of 50 mg/kg. Tumor reductions are found to be associated with increased histone acetylation and decreased HDAC enzyme activity[2].
For CXD101, after oral dosing in murine and canine models, peak plasma concentrations (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-CXD101 at a dose of 1.6 mg/kg (4 μmol/kg), tissue radioactivity peaked 3 to 6 hours after the dose and declined slowly thereafter with CXD101‐related material still present in tissue 21 days after the dose[2].

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

403.52

Formula

C24H29N5O

CAS 号

934828-12-3

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 : ≥ 31 mg/mL (76.82 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4782 mL 12.3910 mL 24.7819 mL
5 mM 0.4956 mL 2.4782 mL 4.9564 mL
10 mM 0.2478 mL 1.2391 mL 2.4782 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.20 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。

    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

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.20 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.20 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]. Eyre TA, et al. Predictive biomarkers for disease sensitivity in lymphoma – the holy grail for HDAC inhibitors? Oncotarget. 2018 Dec 18;9(99):37280-37281.

    [2]. Eyre TA, et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer. 2019 Jan 1;125(1):99-108.

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