BRD4/CK2-IN-1|cas:2756851-99-5|西域试剂

BRD4/CK2-IN-1,98.62%

产品编号：Bellancom-145260| CAS NO：2756851-99-5| 分子式：C₂₉H₃₀ClN₅O₅| 分子量：564.03

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货号	价格	库存与货期
Bellancom-145260	￥2250.00	杭州北京（现货）
Bellancom-145260	￥3420.00	杭州北京（现货）
Bellancom-145260	￥6750.00	杭州北京（现货）
Bellancom-145260	￥10800.00	杭州北京（现货）

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BRD4/CK2-IN-1

产品介绍

BRD4/CK2-IN-1 是一种首次高效、口服有效的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂。BRD4/CK2-IN-1 对 BRD4 和 CK2 的 IC₅₀ 值分别为 180 nM 和 230 nM。BRD4/CK2-IN-1具有很强的抗癌活性，且无明显毒性。BRD4/CK2-IN-1 在三阴性乳腺癌 (TNBC) 中诱导细胞凋亡和自噬相关的细胞死亡。

生物活性

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC₅₀s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)

体外研究

BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC₅₀s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively.
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells.
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3.
BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB.

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

Cell Viability Assay

Cell Line:	MDA-MB-231, MDA-MB-468 cells
Concentration:	0, 0.19, 0.39, 0.78, 1.56, 3.13, 6.25, 12.5, 25 μM
Incubation Time:	24 hours
Result:	Showed anti-proliferative rates in MDA-MB-231 and MDA-MB-468 cells (IC₅₀ = 2.66 and 3.52 μM, respectively).

Apoptosis Analysis

Cell Line:	MDA-MB-231, MDA-MB-468 cells
Concentration:	0, 2.5, 5, 10 μM
Incubation Time:	24 hours
Result:	Dose-dependently induced apoptosis of MDA-MB-231 and MDA-MB-468 cells.

Western Blot Analysis

Cell Line:	MDA-MB-231, MDA-MB-468 cells
Concentration:	0, 2.5, 5, 10 μM
Incubation Time:	24 hours
Result:	Dose-dependently downregulated Bcl-2 but upregulated Bax and cleaved caspase-3.

Cell Line:
Concentration:
Incubation Time:
Result:

体内研究
(In Vivo)

BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models.
BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models.
Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1.

Parameter	iv (1 mg/kg)	po (10 mg/kg)
T_1/2 (h)	4.21±0.57	5.14±0.71
C_max (ng/mL)	237±11	206±6
AUC_0-t (ng·h/mL)	579±49	2079±130
AUC_0-∞ (ng·h/mL)	588±36	2090±146
V_Z (L/kg)	21.1±2.6
CL ((mL/min)/kg)	57.4±1.3
F (%)		32.5

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

Animal Model:	Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells
Dosage:	25 and 50 mg/kg
Administration:	Intragastric administration; daily for 19 days
Result:	Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.

体内研究

Parameter	iv (1 mg/kg)	po (10 mg/kg)
T_1/2 (h)	4.21±0.57	5.14±0.71
C_max (ng/mL)	237±11	206±6
AUC_0-t (ng·h/mL)	579±49	2079±130
AUC_0-∞ (ng·h/mL)	588±36	2090±146
V_Z (L/kg)	21.1±2.6
CL ((mL/min)/kg)	57.4±1.3
F (%)		32.5

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

Animal Model:	Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells
Dosage:	25 and 50 mg/kg
Administration:	Intragastric administration; daily for 19 days
Result:	Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.

体内研究

Parameter	iv (1 mg/kg)	po (10 mg/kg)
T_1/2 (h)	4.21±0.57	5.14±0.71
C_max (ng/mL)	237±11	206±6
AUC_0-t (ng·h/mL)	579±49	2079±130
AUC_0-∞ (ng·h/mL)	588±36	2090±146
V_Z (L/kg)	21.1±2.6
CL ((mL/min)/kg)	57.4±1.3
F (%)		32.5

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

Animal Model:	Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells
Dosage:	25 and 50 mg/kg
Administration:	Intragastric administration; daily for 19 days
Result:	Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (35.46 mM; ultrasonic and warming and adjust pH to 3 with HCl 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	1.7730 mL	8.8648 mL	17.7296 mL
5 mM	0.3546 mL	1.7730 mL	3.5459 mL
10 mM	0.1773 mL	0.8865 mL	1.7730 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