Plogosertib

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Plogosertib

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。

CAS NO:

1137212-79-3

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

CYC140

产品介绍

Plogosertib (CYC140) 是一种选择性的、有效的、具有口服活性的 ATP 竞争性的PLK1抑制剂 (IC₅₀: 3 nM)。Plogosertib 是一种有抗增殖活性的抗癌剂，可用于多种肿瘤的研究，包括食管癌、胃癌、白血病、非小细胞肺癌、卵巢癌和鳞状细胞癌。

生物活性

Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitivePLK1inhibitor (IC₅₀: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lungcancer, ovarian, and squamous cell cancers^[1]^[2].

IC₅₀& Target^[2]

PLK1

3 nM (IC₅₀)

PLK2

149 nM (IC₅₀)

PLK3

393 nM (IC₅₀)

体外研究
(In Vitro)

Plogosertib (CYC140) selectively inhibits PLK1 (IC₅₀: 3 nM), and is >50 fold more potent against PLK2 and PLK3 (IC₅₀s: 149 nM and 393 nM, respectively)^[2].
Plogosertib (0-4 μΜ, 2 h) reduces phosphorylation of the PLK1 substrate, pSer4-nucleophosmin (p-NPM) in KYSE-410 cells^[2].
Plogosertib (100 nM, 24 h) increases in the proportion of mitotic cells, with increased monopolar spindles in HeLa cells^[2].
Plogosertib (72 h) preferentially inhibits cell proliferation in malignant cell lines (IC₅₀s: 14-21 nM), and is less toxic against none-malignant cell lines (IC₅₀: 82 nM)^[2].

Cell Proliferation Assay^[2]

Cell Line:	KYSE-410 cells
Concentration:	0, 0.07, 0.15, 0.3, 0.6, 1.25 μΜ
Incubation Time:	72 h
Result:	Inhibited cell proliferation in a concentration-dependent manner.

Western Blot Analysis^[2]

Cell Line:	KYSE-410 cells
Concentration:	0, 0.01, 0.025, 0.05, 0.1, 0.25, 0.5, 1, 2, 4 μΜ
Incubation Time:	2 h (p-NPM), 24 h (p-HH3), 72 h (cPARP)
Result:	Reduced phosphorylation of the PLK1 substrate (p-NPM). Increased in the mitotic marker pSer10 histone H3 (p-HH3), and the cleavage of PARP (cPARP, an indicator of cell death).

体内研究
(In Vivo)

Plogosertib (CYC140, oral administration, 40 mg/kg, qd 5/2/5) inhibits tumor growth in preclinical xenograft models of acute leukemia and solid tumors^[2]. Plogosertib (Coumpond A7, 1 mg/kg, mouse) shows pharmacokinetic parameters: C_max(453 ng/mL), AUC (377 hrong/mL), Cl (2445 mL/h/kg)^[3].

Animal Model:	HL60 promyelocytic leukemia xenograft^[2]
Dosage:	40, 54, 67 mg/kg, qd 5/2/5
Administration:	Oral administration
Result:	Inhibited tumor growth (>87%) without significant loss in body weight.

Animal Model:	OE19 esophageal xenograft^[2]
Dosage:	40 mg/kg, qd 5/2
Administration:	Oral administration
Result:	Inhibited tumor growth (61 % inhibition).

Clinical Trial

分子量

616.80

Formula

C₃₄H₄₈N₈O₃

CAS 号

1137212-79-3

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.