OP-1074

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。

OP-1074  纯度: 99.47%

OP-1074,纯抗雌激素药,是一种选择性 ER 降解剂 (PA-SERD),对 ERα 和 ERβ 具有特异性抗雌激素活性,可抑制 17β-estradiol (E2)-刺激的转录活性,IC50 分别为 1.6 和 3.2 nM。

OP-1074

OP-1074 Chemical Structure

CAS No. : 1443752-76-8

规格 价格 是否有货 数量
5 mg ¥8500 In-stock
10 mg ¥14500 In-stock
50 mg   询价  
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OP-1074 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively[1].

IC50 & Target[1]

ERα

 

ERβ

 

体外研究
(In Vitro)

OP-1074 (0-100 nM; 24 hours) inhibits  MCF-7 cells  and CAMA-1 cells proliferation with IC50 values of 6.3 and 9.2 nM, respectively[1].
OP-1074 (100 nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells[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.

Cell Viability Assay[1]

Cell Line: MCF-7 cells, CAMA-1 cells
Concentration: 0 nM, 10 nM,100 nM
Incubation Time: 24 hours
Result: Inhibited breast cancer cell proliferation.

Western Blot Analysis[1]

Cell Line: MCF-7 cells, CAMA-1 cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Downregulated ERα protein expression.

分子量

457.56

Formula

C29H31NO4

CAS 号

1443752-76-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

参考文献
  • [1]. Fanning SW, et al. Specific stereochemistry of OP-1074 disrupts estrogen receptor alpha helix 12 and confers pure antiestrogenic activity.Nat Commun. 2018 Jun 18;9(1):2368.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

OP-5244 sodium

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。

OP-5244 sodium 

OP-5244 sodium 是一种有效和具有口服活性的 CD73 抑制剂,IC50 值为 0.25 nM。OP-5244 sodium 通过阻断腺苷的产生来逆转免疫抑制作用,具有进行癌症研究的潜力。

OP-5244 sodium

OP-5244 sodium Chemical Structure

规格 价格 是否有货 数量
5 mg ¥8500 In-stock
10 mg ¥14000 In-stock
25 mg ¥29500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

OP-5244 sodium 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

OP-5244 sodium is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 sodium reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1].

IC50 & Target

IC50: 0.25 nM (CD73)[1]

体外研究
(In Vitro)

OP-5244 inhibits the production of adenosine (ADO), with an EC50 of 0.79±0.38 nM in H1568 (NSCLC) cells[1].
OP-5244 inhibits AMP hydrolysis to ADO in peripheral blood derived CD8+ T cells with an EC50 of 0.22 nM[1].
OP-5244 (4.1-1000 nM; 96 h) rescues AMP-suppressed CD8+ T cells proliferation and cytokine production[1].
OP-5244 (0.01 nM-10 μM) inhibits ADO production completely in human and murine cancer cell lines (H1568 and EMT6, respectively)[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.

体内研究
(In Vivo)

OP-5244 (15 mg/kg/day; s.c. for 13 d) exhibits anti-tumor effects as a single agent as shown by the tumor growth inhibition in mice[1].
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8+ T cells infiltration and reverses immunosuppression in mice[1].
OP-5244 (0.2 mg/kg; i.v.) exhibits terminal elimination half-lives (rat 8.5, dog 0.82, cyno 4.6 h) due to moderate plasma clearance (rat 0.18, dog 1.22, cyno 0.05 L/kg/h) and low steady-state volume of distribution (rat 0.22, dog 0.29, cyno 0.10 L/kg/h)[1].
OP-5244 (10 mg/kg; p.o.) exhibits Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) [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: BALB/c mice with breast cancer[1]
Dosage: 15 mg/kg/day
Administration: S.c. for 13 days
Result: Inhibited tumor growth.
Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group.

分子量

559.87

Formula

C19H28ClN5NaO9P

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

参考文献
  • [1]. Du X, et, al. Orally Bioavailable Small Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression Through Blockade of Adenosine Production. J Med Chem. 2020 Aug 31.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

OP-5244

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。

OP-5244  纯度: 99.63%

OP-5244 是一种有效和具有口服活性的 CD73 抑制剂,IC50 值为 0.25 nM。OP-5244 通过阻断腺苷的产生来逆转免疫抑制作用,具有进行癌症研究的潜力。

OP-5244

OP-5244 Chemical Structure

CAS No. : 2381268-71-7

规格 价格 是否有货 数量
5 mg ¥8500 In-stock
10 mg ¥14000 In-stock
25 mg ¥29500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

OP-5244 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Covalent Screening Library
  • Nucleotide Compound Library
  • Orally Active Compound Library
  • Anti-Lung Cancer Compound Library
  • Targeted Diversity Library

生物活性

OP-5244 is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1].

IC50 & Target

IC50: 0.25 nM (CD73)[1]

体外研究
(In Vitro)

OP-5244 inhibits the production of adenosine (ADO), with an EC50 of 0.79±0.38 nM in H1568 (NSCLC) cells[1].
OP-5244 inhibits AMP hydrolysis to ADO in peripheral blood derived CD8+ T cells with an EC50 of 0.22 nM[1].
OP-5244 (4.1-1000 nM; 96 h) rescues AMP-suppressed CD8+ T cells proliferation and cytokine production[1].
OP-5244 (0.01 nM-10 μM) inhibits ADO production completely in human and murine cancer cell lines (H1568 and EMT6, respectively)[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.

体内研究
(In Vivo)

OP-5244 (15 mg/kg/day; s.c. for 13 d) exhibits anti-tumor effects as a single agent as shown by the tumor growth inhibition in mice[1].
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8+ T cells infiltration and reverses immunosuppression in mice[1].
OP-5244 (0.2 mg/kg; i.v.) exhibits terminal elimination half-lives (rat 8.5, dog 0.82, cyno 4.6 h) due to moderate plasma clearance (rat 0.18, dog 1.22, cyno 0.05 L/kg/h) and low steady-state volume of distribution (rat 0.22, dog 0.29, cyno 0.10 L/kg/h)[1].
OP-5244 (10 mg/kg; p.o.) exhibits Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 µM•h) [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: BALB/c mice with breast cancer[1]
Dosage: 15 mg/kg/day
Administration: S.c. for 13 days
Result: Inhibited tumor growth.
Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group.

分子量

537.89

Formula

C19H29ClN5O9P

CAS 号

2381268-71-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (464.78 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8591 mL 9.2956 mL 18.5912 mL
5 mM 0.3718 mL 1.8591 mL 3.7182 mL
10 mM 0.1859 mL 0.9296 mL 1.8591 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 and light)。-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: ≥ 6.5 mg/mL (12.08 mM); Clear solution

    此方案可获得 ≥ 6.5 mg/mL (12.08 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 65.0 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: ≥ 6.5 mg/mL (12.08 mM); Clear solution

    此方案可获得 ≥ 6.5 mg/mL (12.08 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 65.0 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: ≥ 6.5 mg/mL (12.08 mM); Clear solution

    此方案可获得 ≥ 6.5 mg/mL (12.08 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 65.0 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]. Du X, et, al. Orally Bioavailable Small Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression Through Blockade of Adenosine Production. J Med Chem. 2020 Aug 31.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务