BRD4 Inhibitor-20|cas:2490311-14-1|西域试剂

BRD4 Inhibitor-20,99.00%

产品编号：Bellancom-146208| CAS NO：2490311-14-1| 分子式：C₁₈H₁₈N₂O₄S| 分子量：358.41

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货号	价格	库存与货期
Bellancom-146208	￥1900.00	杭州北京（现货）
Bellancom-146208	￥3100.00	杭州北京（现货）
Bellancom-146208	￥6200.00	杭州北京（现货）
Bellancom-146208	￥9900.00	杭州北京（现货）

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BRD4 Inhibitor-20

产品介绍

BRD4 Inhibitor-20 是一种有效的溴结构域蛋白 4 (BRD4) 抑制剂，具有口服活性。 BRD4 Inhibitor-20 对 BRD4 (BD1) 和BRD4 (BD2) 具有抑制活性，IC₅₀ 值分别为 19 nM 和 28 nM。 BRD4 Inhibitor-20 在癌细胞系中也具有抗增殖活性。 BRD4 Inhibitor-20 可用于结肠癌等多种癌症的研究。

生物活性

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC₅₀ values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.

体外研究

BRD4 Inhibitor-20 (compound 12j) exhibits excellent BRD4 inhibitory activities (BD1, IC₅₀=19 nM; BD2, IC₅₀=28 nM) and inhibitory activities against BRD2 (BD1, IC₅₀=24 nM; BD2, IC₅₀=18 nM).
BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc.
BRD4 Inhibitor-20 (72 h) has anti-proliferation potency with IC₅₀ values of 4.75 μM, 1.35 μM and 44.07 μM in HT-29, HL-60 and WI-38 cells, respectively.
BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase.

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

Western Blot Analysis

Cell Line:	HT-29 cells
Concentration:	0.5, 2.5, 5.0 μM
Incubation Time:	24 h
Result:	Displayed profound inhibitory effects on c-Myc protein expression.

Cell Proliferation Assay

Cell Line:	HT-29, HL-60 and WI-38 cells
Concentration:
Incubation Time:	72 h
Result:	Possessed strong anti-proliferative activity and weak toxicity.

Cell Cycle Analysis

Cell Line:	HT-29 cell lines
Concentration:	2.5, 5.0, 10.0 μM
Incubation Time:	24 h
Result:	Arrested the cell-cycle progression of the cell line into the G1 phases and the percentage of cells in G1 phase after treatment under concentrations of 2.5, 5.0 and 10.0 μM were 85.98%, 86.49% and 86.05%, respectively.

体内研究
(In Vivo)

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie.

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

Animal Model:

rats

Dosage:

5 mg/kg, 15 mg/kg

Administration:

intravenous dosing (iv) or oral dosing (po)

Result:

PK Parameters	iv (5 mg/kg)	po (15 mg/kg)
C_max(μg/L)	-	2175
T_max(h)	-	1.00
t_1/2(h)	1.56	3.59
CL_z/F (L/h/kg)	0.68	1.03
AUC_0−t(μg/L*h)	7296	14384
AUC_0−∞(μg/L*h)	7340	14600
F (%)	-	66%

体内研究

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie.

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

Animal Model:

rats

Dosage:

5 mg/kg, 15 mg/kg

Administration:

intravenous dosing (iv) or oral dosing (po)

Result:

PK Parameters	iv (5 mg/kg)	po (15 mg/kg)
C_max(μg/L)	-	2175
T_max(h)	-	1.00
t_1/2(h)	1.56	3.59
CL_z/F (L/h/kg)	0.68	1.03
AUC_0−t(μg/L*h)	7296	14384
AUC_0−∞(μg/L*h)	7340	14600
F (%)	-	66%

体内研究

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie.

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

Animal Model:

rats

Dosage:

5 mg/kg, 15 mg/kg

Administration:

intravenous dosing (iv) or oral dosing (po)

Result:

PK Parameters	iv (5 mg/kg)	po (15 mg/kg)
C_max(μg/L)	-	2175
T_max(h)	-	1.00
t_1/2(h)	1.56	3.59
CL_z/F (L/h/kg)	0.68	1.03
AUC_0−t(μg/L*h)	7296	14384
AUC_0−∞(μg/L*h)	7340	14600
F (%)	-	66%

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (348.76 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	2.7901 mL	13.9505 mL	27.9010 mL
5 mM	0.5580 mL	2.7901 mL	5.5802 mL
10 mM	0.2790 mL	1.3951 mL	2.7901 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 (protect from light)。-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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献