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BRD4/CK2-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BRD4/CK2-IN-1图片
CAS NO:2756851-99-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

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。
Cas No.2756851-99-5
分子式C29H30ClN5O5
分子量564.03
溶解度DMSO : 20 mg/mL (35.46 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor ofBRD4/CK2(bromodomain-containing protein 4/casein kinase 2), withIC50s 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 inducesapoptosisandautophagy-associated cell death in triple-negative breast cancer (TNBC)[1]

BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect withIC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3[1].
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[1].

Cell Viability Assay[1]

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[1]

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[1]

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:

BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models[1].
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[1].
Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1[1].

Parameteriv (1 mg/kg)po (10 mg/kg)
T1/2(h)4.21±0.575.14±0.71
Cmax(ng/mL)237±11206±6
AUC0-t(ng.h/mL)579±492079±130
AUC0-∞(ng.h/mL)588±362090±146
VZ(L/kg)21.1±2.6
CL ((mL/min)/kg)57.4±1.3
F(%)32.5

Animal Model:Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells[1]
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.