DCZ0415 是一种有效的TRIP13抑制剂，可损害非同源末端连接修复并抑制NF-κB活性。DCZ0415 在体外，体内以及在耐药性骨髓瘤患者衍生的原代细胞中诱导抗骨髓瘤活性。
| 生物活性 | DCZ0415, a potentTRIP13inhibitor, impairs nonhomologous end joining repair and inhibitsNF-κBactivity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | DCZ0415 (10, 20 μM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation[1].
DCZ0415 (1.25-40 μM; 72 hours) induces a significant dose-dependent decrease of viability in
MM cells[1].
DCZ0415 (10, 20 μM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death[1].
DCZ0415 (10, 20 μM; 24 hours) induces a significant accumulation in G0/G1 MM cells[1].
DCZ0415 (10 μM; 48 hours) decreases the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells[1].
DCZ0415 has IC50s of 1.0–10 μM in CalcuSyn in MM cell lines[1].
DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells[1].
Cell Proliferation Assay[1] | Cell Line: | Multiple myeloma (MM) cells | | Concentration: | 10, 20 μM | | Incubation Time: | 72 hours | | Result: | Showed a significant decrease in colony formation, indicating it inhibits cell proliferation. |
Cell Viability Assay[1] | Cell Line: | MM cells | | Concentration: | 1.25, 2.5, 5, 10, 20, 40 μM | | Incubation Time: | 72 hours | | Result: | Induced a significant dose-dependent decrease of viability. |
Apoptosis Analysis[1] | Cell Line: | MM cells | | Concentration: | 10, 20 μM | | Incubation Time: | 24, 48, 72 hours | | Result: | Showed a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death. |
Cell Cycle Analysis[1] | Cell Line: | MM cells | | Concentration: | 10 and 20 μM | | Incubation Time: | 24 hours | | Result: | Induced a significant accumulation in G0/G1 MM cells. |
Western Blot Analysis[1] | Cell Line: | MM cells | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | Decreased the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells. |
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体内研究
(In Vivo) | DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice[1].
| Animal Model: | Nude mice (6-weeks-old) with H929 775 cells[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; every day for 14 days | | Result: | Significantly reduced the growth of MM cells-induced 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 : 62.5 mg/mL(175.35 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8057 mL | 14.0284 mL | 28.0568 mL | | 5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | | 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 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 (5.84 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.84 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.84 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 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: ≥ 2.08 mg/mL (5.84 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.84 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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