Plogosertib CYC140|cas:1137212-79-3|西域试剂

Plogosertib CYC140

产品编号：Bellancom-147298| CAS NO：1137212-79-3| 分子式：C₃₄H₄₈N₈O₃| 分子量：616.80

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-147298	￥2800.00	杭州北京（现货）
Bellancom-147298	￥8200.00	杭州北京（现货）
Bellancom-147298	￥13200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Plogosertib 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-competitive PLK1 inhibitor (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 lung cancer, ovarian, and squamous cell cancers.

体外研究

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).
Plogosertib (0-4 μΜ, 2 h) reduces phosphorylation of the PLK1 substrate, pSer4-nucleophosmin (p-NPM) in KYSE-410 cells.
Plogosertib (100 nM, 24 h) increases in the proportion of mitotic cells, with increased monopolar spindles in HeLa cells.
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).

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

Cell Proliferation Assay

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

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. Plogosertib (Coumpond A7, 1 mg/kg, mouse) shows pharmacokinetic parameters: C_max (453 ng/mL), AUC (377 hr•ng/mL), Cl (2445 mL/h/kg).

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

Animal Model:	HL60 promyelocytic leukemia xenograft
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
Dosage:	40 mg/kg, qd 5/2
Administration:	Oral administration
Result:	Inhibited tumor growth (61 % inhibition).

体内研究

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

Animal Model:	HL60 promyelocytic leukemia xenograft
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
Dosage:	40 mg/kg, qd 5/2
Administration:	Oral administration
Result:	Inhibited tumor growth (61 % inhibition).

体内研究

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

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