DCZ0415 - CAS:2242470-43-3

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DCZ0415

目录号 : KM8425 CAS No. : 2242470-43-3 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg	询价	In-stock

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生物活性

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.

体外研究

DCZ0415 (10, 20 μM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation.
DCZ0415 (1.25-40 μM; 72 hours) induces a significant dose-dependent decrease of viability in MM cells.
DCZ0415 (10, 20 μM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death.
DCZ0415 (10, 20 μM; 24 hours) induces a significant accumulation in G0/G1 MM cells.
DCZ0415 (10 μM; 48 hours) decreases the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells.
DCZ0415 has IC₅₀s of 1.0–10 μM in CalcuSyn in MM cell lines.
DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells.

Cell Proliferation Assay

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

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

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

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

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.

体内研究

DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice.

Animal Model:	Nude mice (6-weeks-old) with H929 775 cells
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; every day for 14 days
Result:	Significantly reduced the growth of MM cells-induced tumors.

分子式

C₂₃H₂₀N₂O₂

分子量

356.42

CAS号

2242470-43-3

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 : 62.5 mg/mL (175.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°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: ≥ 2.08 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-CD in 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 μL 20% 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。