GSK778 - CAS:2451862-42-1

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GSK778 (Synonyms:iBET-BD1)

目录号 : KM11372 CAS No. : 2451862-42-1 纯度 : 98%

Data Sheet 产品使用指南

GSK778 (iBET-BD1) 是一种有效和选择性的 BET 蛋白 BD1 溴结构域的抑制剂，IC₅₀ 值为 75 nM (BRD2 BD1)，41 nM (BRD3 BD1)，41 nM (BRD4 BD1) 和143 nM (BRDT BD1)。GSK778 表型化了 pan-BET 抑制剂在癌症模型中的作用。

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10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC₅₀s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

体外研究

GSK778 inhibits BRD BD2 with the IC₅₀s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively.
GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4 T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22.
GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells.
GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells.
GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells.

Cell Proliferation Assay

Cell Line:	Human primary CD4 T cell
Concentration:	0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Inhibited the proliferative activity of the cells and the production of effector cytokines.

Cell Viability Assay

Cell Line:	MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells
Concentration:	0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	5 days
Result:	Inhibited the growth and viability of human cancer cell lines.

Apoptosis Analysis

Cell Line:	MV4-11, MOLM13, MDA-MB-231 and MB453 cells
Concentration:	1000 nM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation and induced a cell cycle arrest and apoptosis.

体内研究

GSK778 (15 mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model.
GSK778 (15 mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated.
GSK778 exhibits C_max (85 ng/mL), T_max (1.48 h) and AUC_∞ (132 ng.h/mL) following oral administration (10 mg/kg) in mice.

Animal Model:	6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells
Dosage:	15 mg/kg/BID
Administration:	I.p. injections for 30 days
Result:	Increased the survival rate of leukemia mice.

Animal Model:	Male CD1 mice
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o. administration
Result:	C_max (85 ng/mL), T_max (1.48 h); AUC_∞ (132 ng.h/mL).

分子式

C₃₀H₃₃N₅O₃

分子量

511.61

CAS号

2451862-42-1

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 : 41.67 mg/mL (81.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9546 mL	9.7731 mL	19.5461 mL
5 mM	0.3909 mL	1.9546 mL	3.9092 mL
10 mM	0.1955 mL	0.9773 mL	1.9546 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 (4.07 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.07 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 (4.07 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.07 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 (4.07 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.07 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。