计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，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
-20°C储存。超低温运输 。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
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2 , BRD3 , BRD4 ( IC 50 =2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
In Vitro
NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC 50 of 2.46 nM. NHWD-870 (0-10000 nM; 5 dys) suppressed cell growth. NHWD-870 (0-50 nM; 24 hours) inhibits BRD4 phosphorylation and c-MYC expression. NHWD-870 exhibits mild inhibition of hERG channel (IC 50 = 5.4 µM).\nNHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: H526, A2780, ES-2, and MDA-MB231 cells Concentration: 0-10000 nM Incubation Time: 5 days Result: Showed strong inhibitory activities against these cells in 5-day assays. Western Blot AnalysisCell Line: H526, A2780, ES-2, and MDA-MB231 cells Concentration: 0-50 nM Incubation Time: 24 hours Result: Led to the depletion of phosphorylated BRD4 and c-MYC at 10 nM.
In Vivo
NHWD-870 (0.75-3 mg/kg; p.o.) has strong anti-tumor activities in mouse models . NHWD-870 reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation . NHWD-870 manifests diverse mechanisms of action in different cancer settings. These include: 1) inhibition of tumor cell growth by downregulating the PDGFRβ, MEK1/2 and STAT1/MYC signaling in tumor cells; 2) inhibition of tumor angiogenesis by decreasing PDGF production in tumor cells and the PDGFRβ and MEK1/2 signaling in endothelial cells. NHWD-870 has potent tumor suppressive efficacies in xenograft mouse models of small cell lung cancer, triple negative breast cancer and ovarian cancer. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 4-6 weeks old female BALB/c nude mice/6-8 weeks old female C57BL/6 mice were used for B16F10 experiments (bearing NCI-H526, A2780, A375, B16F10, and TMD-8 cells) Dosage: 0.75-3 mg/kg Administration: P.o.; TMD8 and B16F10 melanoma model with once daily for 11-21 days; A375 melanoma and PDX of melanoma with once daily (5 days on, 2 days off) for 21 days. Result: Strongly suppressed the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo.
Form:Solid
规格
规格或纯度
≥99%
英文名称
NHWD-870
生化机理
NHWD-870 是一种强效、口服活性和选择性 BET 家族溴域抑制剂，仅与 BRD2、BRD3、BRD4（IC 50 =2.7 nM）和 BRDT 的溴域结合。NHWD-870 具有强大的抑瘤功效，可抑制癌细胞与巨噬细胞之间的相互作用。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
491.59
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 62.5 mg/mL (127.14 mM; ultrasonic and warming and heat to 60°C)
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:
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。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）