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) |
|---|
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 1 篇同行评审文献引用。
概述
BI 2536是一种有效的Plk1抑制剂，IC50为0.83 nM，比作用于Plk2和Plk3选择性分别高4和11倍。A Plk inhibitor with efficacy against 32 cancer cell lines.
Information
BI-2536 is a potentPlk1inhibitor withIC50of 0.83 nM in a cell-free assay. BI-2536 inhibitsBromodomain 4 (BRD4)with Kd of 37 nM and potently suppressesc-Mycexpression. BI-2536 inducesapoptosisand attenuatesautophagy. Phase 2.
In vitro
BI 2536 blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 nM, respectively. In HeLa cells, BI 2536 treatment ranging from 10-100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, as well as a range of other mitotic processes that are known to depend on Plk1. BI 2536 treatment leads to the HeLa cells arrested in G2/M, subsequently a sub-G1 DNA peak indicative of DNA breakdown and apoptosis, and accumulated cleaved PARP p85 fragments in a concentration-dependent manner. BI 2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM, while blocking the proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells with EC50 of 12-31 nM. Plk1 inhibition by BI 2536 reduces the growth and viability of anaplastic thyroid carcinoma (ATC) cells such as CAL62, OCUT-1, SW1736, 8505C, and ACT-1 with EC50 values of 1.4-5.6 nM.
In vivo
BI 2536 given i.v. once or twice per week is highly efficacious in diverse xenograft models with acceptable tolerability by inhibiting cell proliferation through a mitotic arrest, and subsequently induction of tumor-cell death. Administration of BI 2536 at 50 mg/kg once or twice per week significantly inhibits growth of HCT 116 xenografts with T/C of 15% and 0.3%, respectively. BI 2536 treatment twice-weekly also leads to excellent tumor-growth in BxPC-3 and A549 models with T/C of 5% and 14%, respectively.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~1 μM
Incubation Time：24 and 72 hours
Powder Purity:≥98%
规格
英文别名
(R)-4-(8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
BI 2536
生化机理
BI-2536 是一种强效的 Plk1 抑制剂，在无细胞试验中的 IC50 为 0.83 nM。BI-2536 可抑制 Bromodomain 4 (BRD4)，其 Kd 为 37 nM，并能有效抑制 c-Myc 的表达。BI-2536 可诱导细胞凋亡并抑制自噬。第 2 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 PLK1 抑制剂
名称和识别符
EC号
999-050-2
分子类型
小分子
Isomeric SMILES
CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C
分子量
521.66
Reaxy-Rn
32011809
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=32011809&ln=
技术文档
高级数据
产品属性
| ALogP | 3.7 |
|---|
关联靶点（人）
BRD4
Tchem
含溴结构域蛋白 4(Bromodomain-containing protein 4)
(19 活性数据)
CAMKK2
Tchem
钙/钙调蛋白依赖性蛋白激酶激酶 2(Calcium/calmodulin-dependent protein kinase kinase 2)
(1 活性数据)
PLK3
Tchem
丝氨酸/苏氨酸蛋白激酶 PLK3(Serine/threonine-protein kinase PLK3)
(4 活性数据)
PLK2
Tchem
丝氨酸/苏氨酸蛋白激酶 PLK2(Serine/threonine-protein kinase PLK2)
(4 活性数据)
PLK1
Tchem
丝氨酸/苏氨酸蛋白激酶 PLK1(Serine/threonine-protein kinase PLK1)
(17 活性数据)
BRDT
Tchem
溴结构域睾丸特异性蛋白(Bromodomain testis-specific protein)
(1 活性数据)
CAMKK1
Tchem
钙/钙调蛋白依赖性蛋白激酶激酶 1(Calcium/calmodulin-dependent protein kinase kinase 1)
(1 活性数据)
RPS6KA4
Tchem
核糖体蛋白 S6 激酶 α-4(Ribosomal protein S6 kinase alpha-4)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 48 mg/mL (199.37 mM); Ethanol: 48 mg/mL (199.37 mM); DMSO: 12 mg/mL (49.84 mM);
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）