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  • 化合物 Y06036|T5362|TargetMol

化合物 Y06036|T5362|TargetMol

Y06036
1832671-96-1
￥258 2mg 起订
￥398 5mg 起订
￥663 10mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 Y06036
英文名称：
Y06036
CAS号：
1832671-96-1
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
98.95%
产品类别：
抑制剂
货号：
T5362

Product Introduction

Bioactivity

名称Y06036
描述Y06036, a potent and selective BET inhibitor, can bind to the BRD4(1) bromodomain (Kd: 82 nM).
细胞实验LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells were cultured in RPMI 1640 with 10% FBS at 37 °C and an atmosphere of 5% CO2. For cell viability, cells were seeded in 384-well plates at 500?1000 cells per well (optimum density for growth) in a total volume of 20 μL of media. After 12 h, 10 μL of chemical compounds with 2-fold or 3-fold serial dilution was added to each well with final concentration from 5 nM to 100 μM. The measurement was conducted 96 h after seeded for LNCaP, C4-2B, and 22Rv1 and 144 h after seeded for VCaP. Then, 25 μL of CellTiter-GLO reagents was added, and luminescence was measured on GLOMAX microplate luminometer, according to the manufacturer's instructions. The estimated in vitro half-maximal inhibitory concentration (IC50) values were calculated using Prism 6 software.
动物实验Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) were used for tumor inoculation. Each mouse was inoculated subcutaneously at the dorsal flank on both sides of the mice with C4-2B tumor cells (2 × 10^6 cells) in a mixture of 100 μL PBS and Matrigel (1:1). When the tumor volume reached approximately 100 mm3, the mice were randomized into groups (n = 5?7 per group) and then treated intraperitoneally (ip) with 100 μL of either vehicle or Y06036 and 7m (in a formulation of 15% Cremophor EL, Calbiochem, 82.5% PBS, and 2.5% DMSO) five times per week. The length (L) and width (W) of the tumor mass were monitored by calipers, and volume was expressed in mm3 calculated with the equation V = (π/6)(L × W2). Tumor growth inhibition (TGI) was calculated using the equation TGI = [1 ? (T ? T0)/(C ? C0)] × 100, wherein T and T0 are the mean tumor volumes on a specific experimental day and on the first day of treatment, respectively, for the test groups; and likewise C and C0 are the mean tumor volumes for the vehicle group.
体外活性Y06036与BRD4(1)溴结构域结合，其Kd值为82 nM。Y06036在前列腺癌细胞系中强效抑制细胞增长、集落形成以及AR、AR调控基因和MYC的表达。
体内活性小鼠在肿瘤体积达到约100 mm3时，随机分组并通过腹膜内(i.p.)给药，接受安慰剂或BET抑制剂Y06036（50 mg/kg，每周5次）治疗。在25天的治疗期间，Y06036表现出强大的抗肿瘤活性，肿瘤生长抑制(TGI)达到70%。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 100 mg/mL (234 mM)
关键字inhibit | Epigenetic Reader Domain | Y06036 | Inhibitor | Y 06036 | Y-06036
相关产品Bisdemethoxycurcumin | dBET6 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | CeMMEC1 | (+)-JQ-1 | Curcumin | Naphthol AS-E | J-147 | ABBV-744 | Piflufolastat | Hexamethylene bisacetamide | Anacardic Acid
相关库抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 组蛋白修饰化合物库 | 表观遗传库 | PPI抑制剂库
Y06036|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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