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PLK1/BRD4-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。
PLK1/BRD4-IN-1图片
CAS NO:2412707-81-2
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PLK1/BRD4-IN-1 (9b) 是一个具有口服活性的PLK1和BRD4双重抑制剂，对 PLK1 和 BRD4 的IC50值分别为 22 nM 和 109 nM。PLK1/BRD4-IN-1 诱导细胞周期阻滞 (cell cycle arrest) 和凋亡 (apoptosis)，下调几种增殖相关癌基因的转录，并表现出良好的体内抗肿瘤活性。
生物活性

PLK1/BRD4-IN-1 (9b) is an orally active dualPLK1andBRD4inhibitor withIC50values of 22 nM and 109 nM againstPLK1andBRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest andapoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity[1].

IC50& Target

BRD4

109 nM (IC50)

PLK1

22 nM (IC50)

体外研究
(In Vitro)

PLK1/BRD4-IN-1 (9b) (72 h) shows broad-spectrum antiproliferative activities[1].
PLK1/BRD4-IN-1 (0-9 μM, 24 h) induces cell cycle arrest[1].
PLK1/BRD4-IN-1 (0-9 μM, 48 h) induces cell apoptosis[1].
PLK1/BRD4-IN-1 inhibits the proliferative of cancer cells by exerting its inhibitory activity on both PLK1 and BRD4[1].

Cell Viability Assay[1]

Cell Line:MV4-11, LnCap, HT-29, A375, SKOV-3
Concentration:Cells were maintained in RPMI 1640 or DMEM medium supplemented with 10% FBS (v/v) in 5% CO2, except for MV4-11 cells, which were cultured in IMDM medium.
Incubation Time:72 h
Result:Showed broad-spectrum antiproliferative activities with IC50values of 0.13, 0.14, 1.10, 2.82 and 2.51 μM against MV4-11, LnCap, SKOV-3, A375 and HT29 cells, respectively.

Cell Cycle Analysis[1]

Cell Line:MV4-11
Concentration:0.1, 0.3, 1, 3, 9 μM
Incubation Time:24 h
Result:Induced obvious G2/M arrest in a concentration-dependent manner

Apoptosis Analysis[1]

Cell Line:MV4-11
Concentration:0.1, 0.3, 1, 3, 9 μM
Incubation Time:48 h
Result:Significantly increased the number of Annexin V/PI-positive MV4-11 cells in a concentration-dependent manner.

RT-PCR[1]

Cell Line:MV4-11
Concentration:0.1, 0.3, 1, 3, 9 μM
Incubation Time:24 h
Result:Reduced the transcription of c-MYC and MYCN as well as BCL-2, in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line:MV4-11
Concentration:0.1, 0.3, 1, 3, 9 μM
Incubation Time:48 h
Result:Decreased the expression of c-Myc and Bcl-2 in a concentration dependent-manner and upregulated cleaved caspase-3 and cleaved PARP.
体内研究
(In Vivo)

PLK1/BRD4-IN-1 (9b) (60 mg/kg/d; IG; 18 days) results in a significant decrease in average tumor size, with no obvious toxicity[1].

Animal Model:Five weeks old male NOD-SCID mice[1].
Dosage:60 mg/kg/d
Administration:Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 μL of 1×108cell/mL MV4-11 cell suspension into NOD-SCID mice.
Result:Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice.
分子量

573.73

Formula

C31H43N9O2

CAS 号

2412707-81-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.