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H3B-5942

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产品编号 T5633Cas号 2052128-15-9

H3B-5942 是不可逆的、选择性的、可口服的雌激素受体共价拮抗剂,能够靶作用于 Cys530,使野生型和突变型ERα失活,能够抑制 ERα 的目标基因GREB1的表达。它具有抗癌活性,对含有 ERαWT 或者突变型 ERα 的肿瘤细胞和动物具有抗肿瘤作用。

H3B-5942
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H3B-5942

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纯度: 99.21%
产品编号 T5633Cas号 2052128-15-9

H3B-5942 是不可逆的、选择性的、可口服的雌激素受体共价拮抗剂,能够靶作用于 Cys530,使野生型和突变型ERα失活,能够抑制 ERα 的目标基因GREB1的表达。它具有抗癌活性,对含有 ERαWT 或者突变型 ERα 的肿瘤细胞和动物具有抗肿瘤作用。

规格价格库存数量
1 mg
¥ 313
现货
5 mg
¥ 948
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10 mg
¥ 1,420
现货
25 mg
¥ 2,380
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50 mg
¥ 3,400
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100 mg
¥ 4,600
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200 mg
¥ 6,190
现货
1 mL x 10 mM (in DMSO)
¥ 1,030
现货
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产品介绍

生物活性
产品描述
H3B-5942 belongs to a class of ERα antagonists referred to as selective estrogen receptor covalent antagonists (SERCA).
靶点活性
Erα (Y537S):0.41 nM (Ki), Erα (WT):1 nM (Ki)
体外活性
H3B-5942以30至300 mg/kg的剂量每日一次口服(q.d.×1),在血浆和肿瘤中的暴露量呈剂量成比例的增加,同时ERαY537S/WT ST941肿瘤模型中的ERα靶基因PGR和NPY1R的表达呈剂量成比例的降低。H3B-5942以200 mg/kg的剂量进行单次或重复给药,可以抑制大量直接的ERα靶基因,其中q.d.×1给药能够在给药后最长维持72小时的靶基因抑制效果,且q.d.×3(连续3天每日一次给药)展现出对PGR和NPY1R的最强抑制。
体内活性
单次或重复给予H3B-5942(每次200 mg/kg)能够抑制一大组直接ERα靶基因,其中q.d.×1(每天一次)给药可维持靶基因抑制至多达72小时,而q.d.×3(每天三次)给药在PGR和NPY1R上展现出最强的抑制效果。
激酶实验
ERαWT (297–554) and mutant (297–554) proteins were incubated in 50 mmol/L Tris pH 8.0, 150 mmol/L NaCl, 5% glycerol, and 1 mmol/L TCEP with a 2-fold excess of compound (2 μmol/L H3B-5942:1 μmol/L ERα protein solution) at 4°C overnight.?Mass analyses were carried out (ESI source, 4.0 kV ionization voltage, 250°C capillary temperature, 10 arb sheath gas, S-lens RF level 65) coupled with an Accela Open AS 1250.?Samples (10 μL) were desalted on a C4 column ( 2.1 × 150 mm, 2.6 μm) with a gradient from 5% to 95% B over 10 minutes.?Eluent A consisted of 0.1% formic acid in water, and eluent B consisted of 0.1% formic acid in acetonitrile.?The flow was set to 400 nL/minute.?All solvents were LC/MS grade .?The mass spectrometer was run in positive mode collecting full scan at R = 70,000 from m/z 500 to m/z 2,000.?Data were collected with the Xcalibur 3.1 software.
动物实验
Animals were selected based on TV and randomized into treatment groups of 6 to 8 animals per group.?Single-agent or combination treatments were started on day 0 and continued for the duration of the study.?H3B-5942 was administered orally, tamoxifen was given Q2D, fulvestrant was given?, and palbociclib was administered orally ?Each treatment was administered based on BW (10 mL/kg).?H3B-5942 was formulated daily in 10% 2-Hydroxypropyl-β-CycloDextrin (HPβCD) in 5% dextrose, tamoxifen was formulated in 95% peanut oil/5% ethanol (EtOH), clinical-grade fulvestrant was administered, and palbociclib was formulated in 25 mmol/L sodium bicarbonate, 15 mmol/L lactic acid solution with 2% Cremophor EL.?The BW measurements were performed daily, and tumor measurements were recorded twice a week.
化学信息
分子量494.63
分子式C31H34N4O2
CAS No.2052128-15-9
SmilesCC\C(=C(\c1ccc(OCCNC\C=C\C(=O)N(C)C)cc1)c1ccc2[nH]ncc2c1)c1ccccc1
密度1.157 g/cm3 (Predicted)
储存&溶解度
存储keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (101.09 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.0217 mL10.1086 mL20.2171 mL101.0857 mL
5 mM0.4043 mL2.0217 mL4.0434 mL20.2171 mL
10 mM0.2022 mL1.0109 mL2.0217 mL10.1086 mL
20 mM0.1011 mL0.5054 mL1.0109 mL5.0543 mL
50 mM0.0404 mL0.2022 mL0.4043 mL2.0217 mL
100 mM0.0202 mL0.1011 mL0.2022 mL1.0109 mL

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计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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