计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Adavosertib (MK-1775), 丝氨酸/苏氨酸蛋白激酶 WEE1 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
产品介绍
MK-1775是Wee1的有效选择性抑制剂，无细胞试验中IC50为5.2 nM。MK-1775通过磷酸化Tyr15残基消除细胞周期蛋白依赖性激酶1（CDC2）的活性。Wee1是属于Ser/Thr蛋白激酶家族的核激酶。Wee1激酶通过催化CDC2/cyclin B激酶的抑制性酪氨酸磷酸化，负向调节进入有丝分裂。Wee1的功能紊乱导致小于正常的子细胞的生成。
Information
Adavosertib (MK-1775) Adavosertib (MK-1775, AZD1775) is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint. Phase 2.
In vitro
MK-1775 inhibits Wee1 kinase in an ATP-competitive manner. Compared to Wee1, MK-1775 displays 2- to 3-fold less potency against Yes with IC50 of 14 nM, 10-fold less potency against seven other kinases with >80% inhibition at 1 μM, and >100-fold selectivity over human Myt 1, another kinase that inhibits cyclin-dependent kinase 1 (CDC2) by phosphorylation at an alternative site (Thr14). By abrogating the DNA damage checkpoint via blockade of Wee1 activity in WiDr cells bearing mutated p53, MK-1775 treatment inhibits the basal phosphorylation of CDC2 at Tyr15 (CDC2Y15) with EC50 of 49 nM, and suppresses gemcitabine-, carboplatin- or cisplatin-induced phosphorylation of CDC2 and cell cycle arrest in a dose-dependent manner, with EC50 of 82 nM and 81 nM, 180 nM and 163 nM, as well as 159 nM and 160 nM, respectively. MK-1775 treatment alone at 30-100 nM has no significant antiproliferative effect in WiDr and H1299 cells, whereas MK-1775 at 300 nM, sufficient to inhibit Wee1 by >80%, displays moderate but significant antiproliferative effects by 34.1% in WiDr cells and 28.4% in H1299 cells.
In vivo
MK-1775 treatment alone at ~20 mg/kg displays minimal antitumor effects against WiDr xenografts in rats with T/C of 69% at day 3. Antitumor efficacy by MK-1775 alone in the nude rat HeLa-luc and TOV21G-shp53 xenograft models is also moderate.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：24 hours
Powder Purity:≥98%
规格
别名
阿达沃塞替尼 (MK-1775)
英文别名
AZD1775 | 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-(4-(4-methylpiperazin-1-yl)phenylamino)-1,2-dihydropyrazolo[3,4-d]pyrimidin-3-one
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Adavosertib (MK-1775)
生化机理
Adavosertib （MK-1775，AZD1775）是一种强效的选择性 Wee1 抑制剂，在无细胞试验中的 IC50 为 5.2 nM；可阻碍 G2 DNA 损伤检查点。第二阶段
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/苏氨酸蛋白激酶 WEE1 抑制剂
名称和识别符
EC号
680-342-0
分子类型
小分子
Isomeric SMILES
CC(C)(C1=NC(=CC=C1)N2C3=NC(=NC=C3C(=O)N2CC=C)NC4=CC=C(C=C4)N5CCN(CC5)C)O
分子量
500.61
Reaxy-Rn
12993372
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12993372&ln=
技术文档
高级数据
产品属性
| ALogP | 3.1 |
|---|
关联靶点（人）
JAK3
Tclin
酪氨酸蛋白激酶JAK3(Tyrosine-protein kinase JAK3)
(1 活性数据)
PLK1
Tchem
丝氨酸/苏氨酸蛋白激酶 PLK1(Serine/threonine-protein kinase PLK1)
(1 活性数据)
WEE1
Tchem
Wee1 类蛋白激酶(Wee1-like protein kinase)
(7 活性数据)
WEE2
Tchem
Wee1 类蛋白激酶 2(Wee1-like protein kinase 2)
(2 活性数据)
ADK
Tchem
腺苷激酶(Adenosine kinase)
(1 活性数据)
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:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214613 |
分析证书 | A408386 |
技术文档和文章
溶液计算器
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