IT-901|cas:1584121-99-2|西域试剂

IT-901

产品编号：Bellancom-124179| CAS NO：1584121-99-2| 分子式：C₁₇H₁₄N₂O₄S| 分子量：342.37

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-124179		￥3500.00	杭州北京（现货）
Bellancom-124179		￥5600.00	杭州北京（现货）

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IT-901

产品介绍

IT-901 是一种具有口服活性且有效的 NF-κB 亚基 c-Rel 抑制剂，对 NF-κB 和 c-Rel 与 DNA 结合的 IC₅₀ 分别为 0.1 µM，3 μM。IT-901 是一种具有生物活性的萘硫代巴比妥酸酯衍生物，具有用于人类淋巴瘤和改善移植物抗宿主病 (GVHD) 的潜力。

生物活性

IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC₅₀ of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).

体外研究

IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC and GCB DLBCL cells.
IT-901 (3 μM; for 24 hours) decreases cell viability in a dose-dependent fashion, at least 60 percent of cells were still viable after 48 hours of IT-901 treatment (4μM) in all tested cell lines except HBL1.
IT-901 (1, 5, 10 μM; for 6 hours) documents Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreases the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines.
The IC₅₀ of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM.
The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells.
IT-901 inhibits cell growth of both activated B-like (ABC) and germinal center B-like (GCB) cell lines with the IC₅₀ values between 3μM to 4μM.

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

Cell Proliferation Assay

Cell Line:	TMD8 and SU-DHL8 cells
Concentration:	1, 3, 5 μM
Incubation Time:	For 24 hours
Result:	Resulted in decreased proliferation of viable ABC and GCB DLBCL cells.

Cell Viability Assay

Cell Line:	SU-DHL8 and TMD8 cells
Concentration:	3 μM
Incubation Time:	For 24 hours
Result:	Decreased cell viability in a dose-dependent fashion.

Western Blot Analysis

Cell Line:	Primary chronic lymphocytic leukemia (CLL) cells and cell lines
Concentration:	1, 5, 10 μM
Incubation Time:	For 6 hours
Result:	Documented Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreased the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms.

体内研究
(In Vivo)

IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity.
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T_1/2 and C_max.

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

Animal Model:	BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old
Dosage:	24 mg/kg
Administration:	IP; every other day for 2 weeks
Result:	Had an effective treatment of acute GVHD without impairing anti-tumor activity.

体内研究

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

Animal Model:	BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old
Dosage:	24 mg/kg
Administration:	IP; every other day for 2 weeks
Result:	Had an effective treatment of acute GVHD without impairing anti-tumor activity.

体内研究

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

Animal Model:	BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old
Dosage:	24 mg/kg
Administration:	IP; every other day for 2 weeks
Result:	Had an effective treatment of acute GVHD without impairing anti-tumor activity.

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (36.51 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9208 mL	14.6041 mL	29.2082 mL
5 mM	0.5842 mL	2.9208 mL	5.8416 mL
10 mM	0.2921 mL	1.4604 mL	2.9208 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式