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HDAC1,HDAC2和HDAC3的IC50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。
生物活性 | CXD101 is a potent, selective and orally active class IHDACinhibitor withIC50s of 63 nM, 570 nM and 550 nM forHDAC1,HDAC2andHDAC3, respectively. CXD101 has no activity againstHDACclass II. CXD101 has antitumor activity[1][2]. |
IC50& Target[1] | HDAC1 63 nM (IC50) | HDAC3 550 nM (IC50) | HDAC2 570 nM (IC50) |
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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].
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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‐
elated material still present in tissue 21 days after the dose[2].
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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 |
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溶解性数据 | In Vitro: DMSO : ≥ 31 mg/mL(76.82 mM) *"≥" means soluble, but saturation unknown. 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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本网站选购。
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