(-)-Irofulven MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863|cas:158440-71-2|西域试剂

(-)-Irofulven MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863,98.86%

产品编号：Bellancom-14429| CAS NO：158440-71-2| 分子式：C₁₅H₁₈O₃| 分子量：246.30

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-14429		￥22000.00	杭州北京（现货）

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(-)-Irofulven MGI 114; 6-Hydroxymethylacylfulvene; NSC 683863

产品介绍

(-)-Irofulven (MGI 114) 是一种 Illudin S 类似物，是一种 DNA 烷化剂。(-)-Irofulven 抑制 DNA 复制，诱导肿瘤细胞凋亡 (apoptosis)，并具有有效的抗肿瘤活性。

生物活性

(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.

体外研究

(-)-Irofulven (2.8 μM; 1 hour) induces p53-dependent cell cycle arrest.
(-)-Irofulven (0.8 μM, 0.9 μM and 2.8 μM; 1 hour) induces CHK2 activation is related to p53 status in cells.
(-)-Irofulven inhibits DNA replication and induces chromosome aberrations (breaks and radials).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

Cell Line:	A2780, CAOV3 and HCT116 cells
Concentration:	2.8 μM
Incubation Time:	1 hour
Result:	p53 wild-type cells mainly arrested at G1/S phases, while p53-mutated or p53-null cells arrested at S and G2/M phases.

Western Blot Analysis

Cell Line:	A2780, CAOV3 and HCT116 cells
Concentration:	0.8 μM, 0.9 μM and 2.8 μM
Incubation Time:	1 hour
Result:	Induced the Thr 68 phosphorylation of CHK2 kinase in cells.

体内研究
(In Vivo)

(-)-Irofulven (7 mg/kg; i.p; on days 1-5 and 8-12) produces a statistically significant increase in the median survival of mice bearing tumor cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female athymic BALB/c mice (nu/nu genotype, 6 weeks old or older) injected with human glioblastoma multiforme.
Dosage:	7 mg/kg
Administration:	i.p; on days 1-5 and 8-12
Result:	Was active against all tumor lines.

体内研究

(-)-Irofulven (7 mg/kg; i.p; on days 1-5 and 8-12) produces a statistically significant increase in the median survival of mice bearing tumor cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female athymic BALB/c mice (nu/nu genotype, 6 weeks old or older) injected with human glioblastoma multiforme.
Dosage:	7 mg/kg
Administration:	i.p; on days 1-5 and 8-12
Result:	Was active against all tumor lines.

体内研究

(-)-Irofulven (7 mg/kg; i.p; on days 1-5 and 8-12) produces a statistically significant increase in the median survival of mice bearing tumor cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male and female athymic BALB/c mice (nu/nu genotype, 6 weeks old or older) injected with human glioblastoma multiforme.
Dosage:	7 mg/kg
Administration:	i.p; on days 1-5 and 8-12
Result:	Was active against all tumor lines.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (406.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0601 mL	20.3004 mL	40.6009 mL
5 mM	0.8120 mL	4.0601 mL	8.1202 mL
10 mM	0.4060 mL	2.0300 mL	4.0601 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: ≥ 2.5 mg/mL (10.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.15 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.15 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明