SM-276001 是一种有效的选择性TLR7激动剂,可以诱导抗肿瘤免疫反应。SM-276001 是一种具有口服活性的干扰素 (IFN) 诱导剂。
生物活性 | SM-276001 is a potent selectiveTLR7agonist that can induce antitumor immune responses. SM-276001 is an orally activeinterferon(IFN) inducer[1][2]. |
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体外研究 (In Vitro) | SM-276001 (1 nM-10 μM) dose-dependently activates NF-κB through human TLR7[2].
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体内研究 (In Vivo) | SM-276001 demonstrates potent IFN-inducing activity at a dose of 0.1 mg/kg by oral administration in mice[1]. Oral administration of SM-276001, leads to the induction of an inflammatory cytokine and chemokine milieu and to the activation of a diverse population of immune effector cells including T and B lymphocytes, NK and NKT cells[2]. SM-276001 (3 mg/kg PO biweekly) significantly inhibits tumor growth in the Renca renal cell cancer and CT26 colorectal models[2]. SM-276001 (orally; 0.1, 1 or 10 mg/kg) leads to the activation of a diverse population of spleen-resident immune effector cells in Balb/c and C57BL/6J mice. When administered at 1 mg/kg or greater, the plasma concentration of SM-276001 exceeds the MEC of 30 nM[2].
Animal Model: | C57BL/6 and B6C3F1 mice bearing Renca or CT26 tumors[2] | Dosage: | 3 mg/kg | Administration: | Oral administration twice weekly for 25 days | Result: | Significantly reduced disease burden in mice bearing either Renca or CT26 tumors. |
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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 : 125 mg/mL(381.82 mM;Need ultrasonic) 配制储备液 1 mM | 3.0546 mL | 15.2728 mL | 30.5455 mL | 5 mM | 0.6109 mL | 3.0546 mL | 6.1091 mL | 10 mM | 0.3055 mL | 1.5273 mL | 3.0546 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: ≥ 2.08 mg/mL (6.35 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.35 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。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.35 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.35 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。 *以上所有助溶剂都可在本网站选购。
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