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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Elimusertib (BAY-1895344) hydrochloride, 丝氨酸蛋白激酶 ATR 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
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
Information
Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally availableATRinhibitor with an IC50 of 7 nM.
In vitro
In vitro, BAY 1895344 is shown to be a very potent and highly selective ATR inhibitor (IC50 = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM).
In vivo
BAY 1895344 reveals significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. It also demonstrates very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies. BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥98%
规格
别名
Elimusertib(BAY-1895344)盐酸盐
英文别名
BAY-1895344 HCl | 2-[(3R)-3-methyl-4-morpholinyl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-3-yl)-1,7-Naphthyridine hydrochloride
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Elimusertib (BAY-1895344) hydrochloride
生化机理
Elimusertib（BAY-1895344）盐酸盐是一种强效、高选择性、口服型 ATR 抑制剂，IC50 为 7 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
丝氨酸蛋白激酶 ATR 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@@H]1COCCN1C2=NC3=C(C=CN=C3C4=CC=NN4)C(=C2)C5=CC=NN5C
分子量
375.43
Reaxy-Rn
42843031
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=42843031&ln=
技术文档
高级数据
产品属性
| IC50 | ATR, IC50: 7 nM |
|---|---|
| ALogP | 2.774 |
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 3 |
关联靶点（人）
ATR
Tchem
丝氨酸/苏氨酸蛋白激酶 ATR(Serine/threonine-protein kinase ATR)
(1 活性数据)
MTOR
Tclin
丝氨酸/苏氨酸蛋白激酶 mTOR(Serine/threonine-protein kinase mTOR)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 56 mg/mL (201.22 mM); Water: 56 mg/mL (201.22 mM); Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility
17
DMSO(mM) Max Solubility
45.2814106491223
Water(mg / mL) Max Solubility
＜1
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
溶液计算器
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