GNE-900

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GNE-900

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:

1200126-26-6

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

GNE-900 是一种 ATP 竞争性、选择性和口服活性ChK1抑制剂，对ChKl, ChK2 的IC₅₀值分别为为 0.0011，1.5 μM。GNE-900 废除 G2-M 检查点，增强 DNA 损伤，并诱导胞凋亡 (Apoptosis)。 gemcitabine (HY-17026) 和 GNE-900 给药显示抗肿瘤活性^{[1]< /sup>。}

生物活性

GNE-900 is a an ATP-competitive, selective, and orally activeChK1inhibitor withIC₅₀s of 0.0011, 1.5 μM for ChKl,ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and inducesApoptosis.gemcitabine(HY-17026) and GNE-900 administration shows anti-tumor activity^[1].

IC₅₀& Target^[1]

Chk1

0.0011 μM (IC₅₀)

Chk2

1.5 μM (IC₅₀)

体外研究
(In Vitro)

GNE-900 (1 μM; 1-48 h) 在 HT-29 细胞中与吉西他滨 (50 nM) 联合使用时，可诱导细胞凋亡并增加裂解的 PARP 的表达^[1]。

Apoptosis Analysis^[1]

Cell Line:	HT-29 cells
Concentration:	1 μM
Incubation Time:	1-48 h
Result:	Inducesd apoptosis with increased the expression of cleaved PARP when combination with gemcitabine (50 nM).

体内研究
(In Vivo)

GNE-900 (2.5-40 mg/kg; p.o.; once) 与gemcitabine(HY-17026) 联用能降低肿瘤体积并增加 DNA 损伤和 γ-H2AX 的表达水平在大鼠中^[1]。

Animal Model:	Sprague-Dawley rats (HT-29 tumor xenografts)^[1]
Dosage:	2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg)
Administration:	P.o.; once
Result:	Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels.

分子量

367.45

Formula

C₂₃H₂₁N₅

CAS 号

1200126-26-6

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.