XL413 hydrochloride

CAS: 2062200-97-7 货号: X654780 分子式: C14H13Cl2N3O2 分子量: 326.18
有货
级别和纯度: 10mM in DMSO
储存条件
干燥,-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
X654780-1ml
期货 Stock Image
¥4,880.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7 , with an IC 50 of 3.4 nM, and also shows potent effect with IC 50 s of 215, 42 nM on CK2 , PIM1 , respectively, and an EC 50 of 118 nM on pMCM.

In Vitro

XL413 (BMS-863233) hydrochloride inhibits the cell proliferation (IC 50 =2685 nM), decreases cell viability (IC 50 =2142 nM) and elicits the caspase 3/7 activity (EC 50 =2288 nM) in Colo-205 cells. XL413 hydrochloride also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC 50 =715 nM). XL413 hydrochloride shows cytotoxic effects on tumors, with IC 50 of 22.9 µM in HCC1954 cells and 1.1 µM in Colo-205 cells. XL413 hydrochloride induces apoptosis in the Colo-205 cells, but not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC 50 of 22.7 nM. XL413 hydrochloride is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) hydrochloride is well tolerated at all the doses, with no significant body weight loss . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay

For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC 50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Cdc7 3.4 nM (IC 50 ) PIM1 42 nM (IC 50 ) CK2 215 nM (IC 50 )

规格

别名
XL413盐酸盐
规格或纯度
10mM in DMSO
英文名称
XL413 hydrochloride
生化机理
XL413(BMS-863233)盐酸盐是一种强效、选择性和 ATP 竞争性 Cdc7 抑制剂,IC 50 为 3.4 nM,对 CK2 和 PIM1 的 IC 50 分别为 215 和 42 nM,对 pMCM 的 EC 50 为 118 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
分子量
326.18

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