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PLK1-IN-4
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-IN-4图片
CAS NO:2622273-55-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PLK1-IN-4 是一种有效且具有选择性的PLK1抑制剂,IC50< 0.508 nM。PLK1-IN-4 对多种癌细胞具有广泛的抗增殖活性。PLK1-IN-4 诱导有丝分裂阻滞在 G2/M 期检查点,导致癌细胞凋亡 (apoptosis)。PLK1-IN-4 可用于肝细胞癌的研究。
生物活性

PLK1-IN-4 is a potent and selectivePLK1inhibitor withIC50< 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety ofcancercell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading tocancercellapoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma[1].

IC50& Target

IC50:< 0.508 nM (PLK1)[1]

体外研究
(In Vitro)

PLK1-IN-4 (compound 31) (0-5 μM; 48 hours) exhibits excellent antiproliferative activities against HCC cells[1].
PLK1-IN-4 (60 and 100 nM; 24 hours) induces abnormal spindle formation in HepG2 and HT-29 cells[1].
PLK1-IN-4 (10-300 nM; 0-48 hours) induces apoptosis in cancer cells through G2/M arrest[1].
PLK1-IN-4 (0-120 nM; 24 hours) increases phosphorylation of PLK1, histone H3 and NPM and decreases phosphorylation of Cdc2 in a dose-dependent manner[1].

Cell Proliferation Assay

Cell Line:MDA-MB-231, HeLa, HCT 116, HT-29, HepG2, SMMC7721, A549 ,JeKo-1,K562, Karpas299, A375, DU-145 and L02[1]
Concentration:0-5 μM
Incubation Time:48 hours
Result:Exhibited excellent antiproliferative activities against HCC cells, with IC50s of 11.1 nM and 70.9 nM in HepG2 and SMMC7721 cells.

Cell Cycle Analysis

Cell Line:HepG2[1]
Concentration:10, 30, 60, 100 and 300 nM
Incubation Time:0, 12, 24, 36 and 48 hours
Result:Induced apoptosis in cancer cells through G2/M arrest.

Western Blot Analysis

Cell Line:HepG2[1]
Concentration:0, 10, 30, 60, 90 and 120 nM
Incubation Time:24 hours
Result:Increased phosphorylation of PLK1, histone H3 and NPM and decreased phosphorylation of Cdc2 in a dose-dependent manner.
体内研究
(In Vivo)

PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CLhepof 74.3, 330.9, 61.5 and 196.5 mL/min/kg, respectively[1].
PLK1-IN-4 (30 mg/kg; tail vein injection; once or twice daily, for 12 days) suppresses tumor growth in a dose dependent manner[1].
Pharmacokinetic Parameters of PLK1-IN-4 in male ICR mouse[1].

IV (5 mg/kg)
C0(ng/mL)1790
T1/2(h)1.47
MRT0-inf(h)0.808
MRT0-t(h)0.704
AUC0-t(ng·h/mL)767
AUC0-inf(ng·h/mL)776
CL (mL/min/kg)107
VdSS(L/kg)107

Animal Model:Male nu/nu BALB/c mice (4-6 weeks; injected with HepG2 cells)[1]
Dosage:30 mg/kg
Administration:Tail vein injection; once or twice daily, for 12 days
Result:Suppressed tumor growth in a dose dependent manner, and the tumor growth inhibition (TGI) values were 120.0% and 135.2% at doses of 30 mg/kg once daily and 30 mg/kg twice daily, respectively.
Animal Model:ICR mouse[1]
Dosage:5 mg/kg
Administration:IV; single (Pharmacokinetics Analysis)
Result:Exhibited a short half-life (T1/2) of 1.47 h, moderate exposure with an area under the curve (AUC0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vdss) of 5.21 L/kg.
分子量

550.55

Formula

C24H25F3N6O4S

CAS 号

2622273-55-4

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.