BTdCPU 是一种血红素调节抑制激酶 (HRI) 激活剂,可促进eIF2α磷酸化并诱导Dexamethasone (HY-14648) (Dex) 耐药癌细胞的凋亡。BTdCPU 可用于癌症 (如多发性骨髓瘤和耐 Dex 多发性骨髓瘤) 的研究。
生物活性 | BTdCPU is a potentheme regulated inhibitor kinase(HRI) activator that promoteseIF2αphosphorylation and inducesapoptosisinDexamethasone(HY-14648) (Dex)-resistantcancercells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma[1][2]. |
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体外研究 (In Vitro) | BTdCPU (10 μM; 4, 8 h) BTdCPU induces phosphorylation of eIF2α and promotes cell death in MM cells[1]. BTdCPU (10 μM; 4, 8 h) shows cytotoxic for dex-resistant primary MM cells with relative sparing of normal cells perhaps[1].
Western Blot Analysis[1] Cell Line: | MM1.S and MM1.R cells | Concentration: | 10 μM | Incubation Time: | 0, 4, 8 h | Result: | Induced phosphorylation of eIF2α and upregulated mRNA and protein levels of the pro-apoptotic protein CHOP. |
Western Blot Analysis[1] Cell Line: | Bone marrow mononuclear cells (MNC) from multiple myeloma (MM) patient or healthy donor | Concentration: | 10 μM | Incubation Time: | 0, 4, 8 h | Result: | Induced early expression of CHOP in MM patient cells, but not in healthy bone marrow mononuclear cells (MNC). |
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体内研究 (In Vivo) | BTdCPU (175 mg/kg; i.p.; single daily for 21 days) inhibits tumor growth without toxicity in mice xenograft breast tumors model[2].
Animal Model: | Female nude mice (mice xenograft breast tumors model)[2]. | Dosage: | 175 mg/kg | Administration: | Intraperitoneal injection; single daily for 21 days | Result: | Led to complete tumor stasis,which persisted for the remainder of the 3-week study Showed good safety in mice. |
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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(368.51 mM;Need ultrasonic) 配制储备液 1 mM | 2.9481 mL | 14.7406 mL | 29.4811 mL | 5 mM | 0.5896 mL | 2.9481 mL | 5.8962 mL | 10 mM | 0.2948 mL | 1.4741 mL | 2.9481 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: ≥ 2.17 mg/mL (6.40 mM); Clear solution
此方案可获得 ≥ 2.17 mg/mL (6.40 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 21.7 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 (6.13 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.13 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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