标签归档：dimer

Ibrutinib dimer(Synonyms: 依鲁替尼二聚体)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Ibrutinib dimer (Synonyms: 依鲁替尼二聚体)

Ibrutinib dimer 是 Ibrutinib 的二聚体。Ibrutinib dimer 是 Ibrutinib 的一种杂质。Ibrutinib 是一种不可逆的选择性 Btk 抑制剂，IC50 为 0.5 nM。

Ibrutinib dimer(Synonyms: 依鲁替尼二聚体)

Ibrutinib dimer Chemical Structure

CAS No. : 2031255-23-7

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生物活性

Ibrutinib dimer is a Dimer of Ibrutinib. Ibrutinib dimer is an impurity of Ibrutinib[1]. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM[2].

分子量

880.99

Formula

C50H48N12O4
CAS 号

2031255-23-7
中文名称

依鲁替尼二聚体
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Somana Siva Prasad, et al. A QUALITY BY DESIGN APPROACH FOR DEVELOPMENT OF SIMPLE AND ROBUST REVERSED PHASE STABILITY INDICATING HPLC METHOD FOR ESTIMATION OF IBRUTINIB AND ITS IMPURITIES.

    [2]. Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80.

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Anastrozole-d3 Dimer Impurity(Synonyms: 阿那曲唑二聚体杂质 d3)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Anastrozole-d3 Dimer Impurity (Synonyms: 阿那曲唑二聚体杂质 d3)

Anastrozole-d3 Dimer Impurity 是 Anastrozole 的氘代物。Anastrozole 是一种选择性的芳香酶 (aromatase) 抑制剂，抑制胎盘芳香化酶，IC50 为 15 nM。

Anastrozole-d3 Dimer Impurity(Synonyms: 阿那曲唑二聚体杂质 d3)

Anastrozole-d3 Dimer Impurity Chemical Structure

CAS No. : 1329809-14-4

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10 mg Check price and availability

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生物活性

Anastrozole-d3 Dimer Impurity is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

520.65

Formula

C30H28D3N9
CAS 号

1329809-14-4
中文名称

阿那曲唑二聚体杂质 d3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Dukes M, et al. The preclinical pharmacology of “Arimidex” (anastrozole; ZD1033)–a potent, selective aromatase inhibitor. J Steroid Biochem Mol Biol. 1996 Jul;58(4):439-45.

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MSA-2 dimer

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MSA-2 dimer  纯度: 98.44%

MSA-2 dimer 是一种具有选择性和口服活性的非核苷酸 STING 激动剂 (Kd=145 μM)，有长期抗肿瘤和免疫原活性。MSA-2 dimer 作为非共价二聚体与 STING 结合，其渗透率高于循环二核苷酸。

MSA-2 dimer

MSA-2 dimer Chemical Structure

CAS No. : 2377881-92-8

规格 价格 是否有货 数量
5 mg ￥8500 In-stock
10 mg ￥13500 In-stock
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100 mg   询价  

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MSA-2 dimer 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1].

IC50 & Target

Kd: 145 μM (STING)[1]
体内研究
(In Vivo)

MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1].
MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].
MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1].
MSA-2 dimer (60 mg/kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues [1].
MSA-2 dimer (THP-1 cells) induces phosphorylation of both TBK1 and IR. MSA-2 dimer (10 μM and 33 μM; macrophages) induces IFN-β[1].
MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B16F10 tumor-bearing mice
Dosage: 60 mg/kg
Administration: P.o.; 50 days
Result: Inhibited tumor growth and prolonged overall survival.
Animal Model: C57BL6 mice
Dosage: 40 mg/kg
Administration: S.c.; 25 days
Result: Induced complete tumor regression.
Animal Model: C57BL6 mice
Dosage: 60 mg/kg
Administration: P.o.; 4 hours
Result: Increased proinflammatory cytokine (IFN-β) level in tumors.
Animal Model: C57BL6 mice
Dosage: 50 mg/kg
Administration: S.c.; 4 hours
Result: MSA-2 concentrations were observed in tumors than in plasma or other nontumor tissues.

分子量

568.66

Formula

C29H28O8S2
CAS 号

2377881-92-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 70 mg/mL (123.10 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7585 mL 8.7926 mL 17.5852 mL
5 mM 0.3517 mL 1.7585 mL 3.5170 mL
10 mM 0.1759 mL 0.8793 mL 1.7585 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.75 mg/mL (3.08 mM); Clear solution

    此方案可获得 ≥ 1.75 mg/mL (3.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 17.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.75 mg/mL (3.08 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.75 mg/mL (3.08 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 17.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.75 mg/mL (3.08 mM); Clear solution

    此方案可获得 ≥ 1.75 mg/mL (3.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 17.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.

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