PD-1/PD-L1-IN-27

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。

PD-1/PD-L1-IN-27 

PD-1/PD-L1-IN-27 是一种有效的 PD-1/PD-L1 抑制剂,IC50 值为 134 nM。 PD-1/PD-L1-IN-27 具有低 T 细胞毒性的抗肿瘤作用。PD-1/PD-L1-IN-27 具有激活 CD8+ T 细胞和减少 T 细胞耗竭的能力。

PD-1/PD-L1-IN-27

PD-1/PD-L1-IN-27 Chemical Structure

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生物活性

PD-1/PD-L1-IN-27 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 134 nM. PD-1/PD-L1-IN-27 shows antitumor effects with low T cell cytotoxicity. PD-1/PD-L1-IN-27 has the ability to activate CD8+ T cells and reduces T cell exhaustion[1].

IC50 & Target

IC50: 134 nM (PD-1/PD-L1)[1]

体外研究
(In Vitro)

PD-1/PD-L1-IN-27 (compound MZ58) (2.5, 5, 10, 50 µM; 48 h) shows antitumor effects with low T cell cytotoxicity[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5, 5, 10, 50 µM
Incubation Time: 48 h
Result: Facilitated cell proliferation with low T cell cytotoxicity.

体内研究
(In Vivo)

PD-1/PD-L1-IN-27 (10, 25 mg/kg; i.g.) shows antitumor effecct[1].

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

Animal Model: 20-22 g, 6-8 weeks, male C57BL/6J mice (MC 38 cell lines)[1]
Dosage: 10, 25 mg/kg
Administration: I.g.
Result: Showed antitumor effecct.

分子量

673.75

Formula

C44H35NO6

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]. Zhang M, et al. Molecular hybridization used to design and synthesize neo-tanshinlactone derivatives as PD-1/PD-L1 inhibitors. Bioorg Med Chem. 2022; 54:116579.

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Fraxinellone

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。

Fraxinellone  纯度: 99.99%

Fraxinellone 是从芸苔科植物 Dictamnus dasycarpus 的根皮中分离出来的。 Fraxinellone 是 PD-L1 抑制剂,可抑制 HIF-1α 蛋白质合成,而不会影响 HIF-1α 蛋白质降解。 Fraxinellone 通过靶向 PD-L1,有用于癌症免疫的潜能。

Fraxinellone

Fraxinellone Chemical Structure

CAS No. : 28808-62-0

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生物活性

Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1[1].

体外研究
(In Vitro)

Fraxinellone (0-100 μM;12 hours) decreases the percent of PD-L1 positive cells from 20.4% to 11.4% in A549 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: A549 cells
Concentration: 0 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 12 hours
Result: Inhibited the percent of PD-L1 positive cells.

体内研究
(In Vivo)

Fraxinellone (oral gavage; 30 and 100 mg/kg; every three days; 30 days) significantly suppresses tumor growth, reduces HIF-1α, pTyr705 STAT3, PD-L1 and VEGF staining compared with the control group in female athymic BALB/c nude mice[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 nude mice[1]
Dosage: 30 and 100 mg/kg
Administration: Oral gavage; 30 and 100 mg/kg; every three days; 30 days
Result: Significantly suppressed tumor growth.

分子量

232.28

Formula

C14H16O3

CAS 号

28808-62-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (430.51 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3051 mL 21.5257 mL 43.0515 mL
5 mM 0.8610 mL 4.3051 mL 8.6103 mL
10 mM 0.4305 mL 2.1526 mL 4.3051 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。-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: ≥ 2.5 mg/mL (10.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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% corn oil

    Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.76 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 25.0 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]. Xing Y, et al. Fraxinellone has anticancer activity in vivo by inhibiting programmed cell death-ligand 1 expression by reducing hypoxia-inducible factor-1α and STAT3. Pharmacol Res. 2018 Sep;135:166-180.

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INCB086550(Synonyms: PD-1/PD-L1-IN-8)

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。

INCB086550 (Synonyms: PD-1/PD-L1-IN-8) 纯度: 98.86%

INCB086550 (PD-1/PD-L1-IN-8; example 24) 是 PD-1/PD-L1 的抑制剂,其IC50 值为 <= 10 nM。

INCB086550(Synonyms: PD-1/PD-L1-IN-8)

INCB086550 Chemical Structure

CAS No. : 2230911-59-6

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生物活性

INCB086550 (PD-1/PD-L1-IN-8; example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM[1].

分子量

693.79

Formula

C41H39N7O4

CAS 号

2230911-59-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 83.33 mg/mL (120.11 mM; ultrasonic and adjust pH to 3 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4414 mL 7.2068 mL 14.4136 mL
5 mM 0.2883 mL 1.4414 mL 2.8827 mL
10 mM 0.1441 mL 0.7207 mL 1.4414 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。-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。

参考文献
  • [1]. WU LIANGXING, et al. BENZOOXAZOLE DERIVATIVES AS IMMUNOMODULATORS. WO2018119266A1.

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Camrelizumab(Synonyms: 卡瑞利珠单抗; SHR-1210)

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。

Camrelizumab (Synonyms: 卡瑞利珠单抗; SHR-1210) 纯度: 97.70%

Camrelizumab (SHR-1210) 是一种人源化的 IgG4-κ 抗 PD-1 单克隆抗体 (mAb)。Camrelizumab 以 3 nM 的高亲和力与 PD-1 结合,抑制 PD-1 和 PD-L1 的结合作用的 IC50 值为 0.70 nM。Camrelizumab 是一种有效的抗 PD-1/PD-L1 药物,可用于癌症研究,包括非小细胞肺癌、食管鳞状细胞癌、霍奇金淋巴瘤和晚期肝癌等。

Camrelizumab(Synonyms: 卡瑞利珠单抗; SHR-1210)

Camrelizumab Chemical Structure

CAS No. : 1798286-48-2

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生物活性

Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al[1][2].

IC50 & Target

IC50: 0.70 nM ( PD-1/PD-L1 interaction)[1]

体外研究
(In Vitro)

In a T cell proliferation assay using tuberculin treated peripheral blood mononuclear cells, Camrelizumab induces a T cell proliferation at an EC50 of 0.11 nM. In a similar assay measuring IFN-gamma secretion, Camrelizumab induces IFN-gamma production at an EC50 of 0.38 nM[2].

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)

Camrelizumab (3 mg/kg) combines with apatinib (200 and 100 mg/kg) inhibits the tumor inhibition rates reached 63.1% and 87.3%, respectively in human PD-1 transgenic mice[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.

Clinical Trial

CAS 号

1798286-48-2

中文名称

卡瑞利珠单抗

储存方式

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

参考文献
  • [1]. Kuimin Mei, et al. Camrelizumab in combination with apatinib in second-line or above therapy for advanced primary liver cancer: cohort A report in a multicenter phase Ib/II trial. J Immunother Cancer. 2021 Mar;9(3):e002191.

    [2]. Jason D Lickliter, et al.A First-in-Human Dose Finding Study of Camrelizumab in Patients with Advanced or Metastatic Cancer in Australia. Drug Des Devel Ther

    [3]. Caicun Zho, et al.Camrelizumab plus carboplatin and pemetrexed versus chemotherapy alone in chemotherapy-naive patients with advanced non-squamous non-small-cell lung cancer (CameL): a randomised, open-label, multicentre, phase 3 trial. Lancet Respir Med. 2021 Mar;9(3):305-314.

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PD153035 Hydrochloride(Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride)

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。

PD153035 Hydrochloride (Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride) 纯度: 99.06%

PD153035 Hydrochloride (SU-5271 Hydrochloride) 是有效地 EGFR 抑制剂,KiIC50 值分别为6和25 pM。

PD153035 Hydrochloride(Synonyms: SU-5271 Hydrochloride; AG1517 Hydrochloride; ZM 252868 Hydrochloride)

PD153035 Hydrochloride Chemical Structure

CAS No. : 183322-45-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥663 In-stock
50 mg ¥2480 In-stock
100 mg ¥4200 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

PD153035 Hydrochloride (SU-5271 Hydrochloride) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.

IC50 & Target

EGFR

6 pM (Ki)

EGFR

25 pM (IC50)

体外研究
(In Vitro)

PD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM[1]. PD153035 has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD153035 rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation[2]. PD153035 causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC50 is less than 1 pM in most cases[3].

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)

PD153035 levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD 153035 falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors[4].

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.

分子量

396.67

Formula

C16H15BrClN3O2

CAS 号

183322-45-4

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 : 5.125 mg/mL (12.92 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5210 mL 12.6049 mL 25.2099 mL
5 mM 0.5042 mL 2.5210 mL 5.0420 mL
10 mM 0.2521 mL 1.2605 mL 2.5210 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。

参考文献
  • [1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.

    [2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.

    [3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.

    [4]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302.

Cell Assay
[3]

Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed[3].

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 Administration
[3]

Mice: Mice are injected with PD153035 (80 mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD 153035 of the EGF-stimulation[3].

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.

参考文献
  • [1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.

    [2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5.

    [3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.

    [4]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302.

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PD318088

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。

PD318088  纯度: 99.88%

PD318088 是一种有效的、变构的、非 ATP 竞争性的 MEK1/2 抑制剂,PD184352 (HY-50295) 的结构类似物。PD318088 在MEK1 活性位点与 ATP 结合位点相邻的区域与 ATP 同时结合。PD318088 可用于癌症研究。

PD318088

PD318088 Chemical Structure

CAS No. : 391210-00-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1562 In-stock
5 mg ¥1265 In-stock
10 mg ¥2380 In-stock
50 mg ¥7217 In-stock
100 mg ¥10500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research[1].

IC50 & Target[1][2]

MEK1

 

MEK2

 

体外研究
(In Vitro)

PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates[1].
The mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure[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.

分子量

561.09

Formula

C16H13BrF3IN2O4

CAS 号

391210-00-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (178.22 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7822 mL 8.9112 mL 17.8225 mL
5 mM 0.3564 mL 1.7822 mL 3.5645 mL
10 mM 0.1782 mL 0.8911 mL 1.7822 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。-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: ≥ 2.75 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (4.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 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: ≥ 2.75 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (4.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 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: ≥ 2.75 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (4.90 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 27.5 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]. Ohren JF, et al. Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7.

    [2]. Han S, et al. Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5467-73.

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Palbociclib-d8(Synonyms: PD 0332991-d8)

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。

Palbociclib-d8 (Synonyms: PD 0332991-d8) 纯度: 99.84%

Palbociclib D8 (PD 0332991 D8) 是 Palbociclib 的氘代物。Palbociclib 是一种选择性的口服活性的 CDK4CDK6 抑制剂,IC50 分别为 11 nM 和 16 nM。Palbociclib 有潜力用于 ER 阳性和 HER2 阴性乳腺癌的研究。

Palbociclib-d8(Synonyms: PD 0332991-d8)

Palbociclib-d8 Chemical Structure

CAS No. : 1628752-83-9

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生物活性

Palbociclib D8 (PD 0332991 D8) is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].

IC50 & Target

Cdk4/cyclin D3

9 nM (IC50)

Cdk4/cyclin D1

11 nM (IC50)

Cdk6/cyclin D2

16 nM (IC50)

DYRK1A

2000 nM (IC50)

MAPK

8000 nM (IC50)

分子量

455.58

Formula

C24H21D8N7O2

CAS 号

1628752-83-9

中文名称

帕布昔利布 d8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.

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Zapnometinib(Synonyms: PD0184264; ATR-002)

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。

Zapnometinib (Synonyms: PD0184264; ATR-002) 纯度: 99.63%

Zapnometinib (PD0184264) 是 CI-1040 的活性代谢物,是一种 MEK 抑制剂,IC50 值为 5.7 nM。Zapnometinib 具有抗流感病毒的抗病毒活性和抗菌活性。

Zapnometinib(Synonyms: PD0184264;  ATR-002)

Zapnometinib Chemical Structure

CAS No. : 303175-44-2

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  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities[1][2][3].

IC50 & Target[1]

MEK

5.7 nM (IC50)

体外研究
(In Vitro)

Zapnometinib (0.1 nM-1 μM) inhibits MEK, with IC50s of 30.96 nM, 357 nM, and 15 nM in cell free kinase assay, A549, MDCK cells and human PBMCs[1].
Zapnometinib (100 μM; 4 h) inhibits the Ionomycin (PMA/I)-induced phosphorylation of ERK1/2 in human PBMCs[1].
Zapnometinib (1-100 μM) reduces the viral titers of the IV H1N1pdm09, H3N2[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.

Western Blot Analysis[1]

Cell Line: human PBMCs
Concentration: 100 μM
Incubation Time: 4 h
Result: Inhibited the Ionomycin (PMA/I)-increased pERK1/2.

体内研究
(In Vivo)

Zapnometinib (8.4-75 mg/kg/day; three times a day p.o.) reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection[1].
Zapnometinib (150 mg/kg) exhibits AUC values of 860.02 and 1953.68 μg•h/mL in mice by i.v. or oral route, 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.

Animal Model: Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09[1]
Dosage: 8.4, 25, 75 mg/kg/day (2.8, 8.4, 25 mg/kg)
Administration: P.o. three times a day
Result: Significantly reduced the virus titer at the dose of either 75 mg/kg/day or 25 mg/kg/day.

分子量

409.55

Formula

C13H7ClF2INO2

CAS 号

303175-44-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (152.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4417 mL 12.2085 mL 24.4170 mL
5 mM 0.4883 mL 2.4417 mL 4.8834 mL
10 mM 0.2442 mL 1.2209 mL 2.4417 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 (protect from 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: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.08 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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% corn oil

    Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.08 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 20.8 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]. Laure M, et, al. Antiviral efficacy against influenza virus and pharmacokinetic analysis of a novel MEK-inhibitor, ATR-002, in cell culture and in the mouse model. Antiviral Res. 2020 Jun;178:104806.

    [2]. Hamza H, et, al. Improved in vitro Efficacy of Baloxavir Marboxil Against Influenza A Virus Infection by Combination Treatment With the MEK Inhibitor ATR-002. Front Microbiol. 2021 Feb 12;12:611958.

    [3]. Bruchhagen C, et, al. Metabolic conversion of CI-1040 turns a cellular MEK-inhibitor into an antibacterial compound. Sci Rep. 2018 Jun 14;8(1):9114.

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PD-1/PD-L1-IN-9

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。

PD-1/PD-L1-IN-9  纯度: 98.01%

PD-1/PD-L1-IN-9 是一种有效和具有口服活性的 PD-1/PD-L1 相互作用抑制剂,IC50 值为 3.8 nM。PD-1/PD-L1-IN-9 可以增强免疫细胞对肿瘤细胞的杀伤活性。PD-1/PD-L1-IN-9 在 CT26 小鼠模型中表现出显着的体内抗肿瘤活性。

PD-1/PD-L1-IN-9

PD-1/PD-L1-IN-9 Chemical Structure

CAS No. : 2628506-54-5

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生物活性

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model[1].

IC50 & Target

IC50: 3.8 nM (PD-1/PD-L1)[1]

体外研究
(In Vitro)

PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of PBMCs to MDB-MB 231 cells, with an EC50 of ∼100 nM[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)

PD-1/PD-L1-IN-9 (compound 24) (40-80 mg/kg; p.o. once a day for 2 weeks) inhibits tumor growth in a dose-dependent manner and does not cause any body weight loss or mortality of mice[1].
PD-1/PD-L1-IN-9 (3 mg/kg; a single i.v.) exhibits half-life (t1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats[1].
PD-1/PD-L1-IN-9 (25 mg/kg; a single p.o.) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[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: Male BALB/c mice (5-6 weeks) were inoculated CT26 cells[1]
Dosage: 40, 80 mg/kg
Administration: P.o. once a day for 2 weeks
Result: Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 3 mg/kg for i.v. and 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: A single i.v. or p.o.
Result: I.v.: t1/2=4.2 h; Cl=11.5 L/h/kg; Cmax=1233 ng/mL.
P.o.: F=22 %; t1/2=6.4 h; Cmax=192 ng/mL.

分子量

348.44

Formula

C22H24N2O2

CAS 号

2628506-54-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (286.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8699 mL 14.3497 mL 28.6993 mL
5 mM 0.5740 mL 2.8699 mL 5.7399 mL
10 mM 0.2870 mL 1.4350 mL 2.8699 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。-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: ≥ 2.5 mg/mL (7.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (7.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.17 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 25.0 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]. Wang T, et, al. Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction. J Med Chem. 2021 May 30.

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TPP-1

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。

TPP-1  纯度: 98.04%

TPP-1 是 PD-1/PD-L1 相互作用的有效抑制剂。TPP-1 与 PD-L1 特异性高亲和力结合 (KD=95 nM)。动物模型中,TPP-1 通过再激活 T 细胞功能抑制肿瘤生长。

TPP-1

TPP-1 Chemical Structure

CAS No. : 2426685-25-6

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50 mg   询价  
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TPP-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function[1].

体外研究
(In Vitro)

TPP-1 binds to PD-L1 with high affinity and blocks PD-1/PD-L1 interaction. The KD value of PD-L1 with TPP-1 peptide is about 95 nmol/L (around five times less than that with PD-1), The binding site of TPP-1 to PD-L1 is close to the interactive site of PD-1 and PD-L1[1].
TPP-1 (4 μM) reactivates T-cell functions, it induces IFNγ release significantly higher than control and SPP-1, and the TPP-1 group shows similar outcomes for cell proliferation[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)

TPP-1 (subcutaneous injection; 4 mg/kg; every other day eight times; 32 days) inhibits tumor growth (compared with SPP-1 and control). The growth rate in TPP-1-treated mice is 56%. And when administered in the absence of T cells (control group), TPP-1 has no effect on the growth of the H460-luc tumors[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: 5 to 6-week-old female Balb/c nude mice  injected with H460 cells transfected with the plvx-puro/luciferase lentiviral vector[1]
Dosage: 4 mg/kg
Administration: Subcutaneous injection; 4 mg/kg; every other day eight times; 32days
Result: Inhibited the tumor growth in a tumor xenograft model via reactivating T-cell function. 

分子量

2488.67

Formula

C107H150N34O32S2

CAS 号

2426685-25-6

Sequence Shortening

SGQYASYHCWCWRDPGRSGGSK

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 50 mg/mL (20.09 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.4018 mL 2.0091 mL 4.0182 mL
5 mM 0.0804 mL 0.4018 mL 0.8036 mL
10 mM 0.0402 mL 0.2009 mL 0.4018 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。-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。

参考文献
  • [1]. Chunlin Li, et al. Peptide Blocking of PD-1/PD-L1 Interaction for Cancer Immunotherapy. Cancer Immunol Res. 2018 Feb;6(2):178-188.

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PD-161570

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。

PD-161570  纯度: 99.04%

PD-161570 是一种有效的且具有 ATP 竞争能力的人 FGF-1 受体抑制剂,IC50 为 39.9 nM,Ki 为 42 nM。PD-161570 还抑制 PDGFREGFRc-Src 酪氨酸激酶,IC50 值分别为 310 nM,240 nM 和 44 nM。PD-161570 抑制 PDGF 刺激的自磷酸化和 FGF-1 受体磷酸化,IC50 分别为 450 nM 和 622 nM。PD-161570 还是一种骨形态发生蛋白 (BMPs) 和 TGF-β 信号抑制剂。

PD-161570

PD-161570 Chemical Structure

CAS No. : 192705-80-9

规格 价格 是否有货 数量
5 mg ¥2500 In-stock
10 mg ¥4000 In-stock
50 mg   询价  
100 mg   询价  

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PD-161570 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • TGF-beta/Smad Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively[1][2]. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor[3].

IC50 & Target[1][2][3]

FGFR1

39.9 nM (IC50)

FGFR1

42 nM (Ki)

FGFR1 autophosphorylation

622 nM (IC50)

PDGFRβ

262 nM (IC50)

PDGFR

310 nM (IC50)

EGFR

240 nM (IC50)

c-Src

44 nM (IC50)

TGF-β Receptor

 

体外研究
(In Vitro)

PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC50 of 0.3 µM on day 8[1].
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture[2].
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis[4].

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 Proliferation Assay[1]

Cell Line: Vascular smooth muscles cells (VSMCs)
Concentration: 0.1 µM, 0.3 µM, 1 µM
Incubation Time: 1 day, 3 days, 6 days, 8 days
Result: Inhibited VSMC proliferation in a dose dependent fashion with an IC50 of 0.3 µM at day 8.

分子量

532.51

Formula

C26H35Cl2N7O

CAS 号

192705-80-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (62.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8779 mL 9.3895 mL 18.7790 mL
5 mM 0.3756 mL 1.8779 mL 3.7558 mL
10 mM 0.1878 mL 0.9389 mL 1.8779 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。-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。

参考文献
  • [1]. Hamby JM, et al. Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. J Med Chem. 1997 Jul 18;40(15):2296-303.

    [2]. Batley BL, et al. Inhibition of FGF-1 receptor tyrosine kinase activity by PD 161570, a new protein-tyrosine kinase inhibitor. Life Sci. 1998;62(2):143-50.

    [3]. Kyosuke Hino, et al. An mTOR Signaling Modulator Suppressed Heterotopic Ossification of Fibrodysplasia Ossificans Progressiva. Stem Cell Reports. 2018 Nov 13;11(5):1106-1119.

    [4]. Wolfe A, et al. Pharmacologic characterization of a kinetic in vitro human co-culture angiogenesis model using clinically relevant compounds. J Biomol Screen. 2013 Dec;18(10):1234-45.

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PD-1-IN-17

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。

PD-1-IN-17  纯度: ≥95.0%

PD-1-IN-17 是一种有效的程序性细胞死亡-1 (PD-1) 抑制剂,详细信息请参考专利文献 WO2015033301A1 中的化合物 12,浓度为 100 nM 时抑制 92% 脾细胞增殖。

PD-1-IN-17

PD-1-IN-17 Chemical Structure

CAS No. : 1673560-66-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5280 In-stock
5 mg ¥4800 In-stock
10 mg ¥8000 In-stock
25 mg ¥15500 In-stock
50 mg ¥24000 In-stock
100 mg ¥36000 In-stock
200 mg   询价  
500 mg   询价  

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PD-1-IN-17 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM[1].

IC50 & Target

PD-1[1]

分子量

374.35

Formula

C13H22N6O7

CAS 号

1673560-66-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 125 mg/mL (333.91 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6713 mL 13.3565 mL 26.7130 mL
5 mM 0.5343 mL 2.6713 mL 5.3426 mL
10 mM 0.2671 mL 1.3356 mL 2.6713 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: ≥ 2.08 mg/mL (5.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.56 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.56 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.56 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 20.8 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]. Pottayil Govindan Nair Sasikumar, et al. 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives as immunomodulators. WO2015033301A1.

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Nevanimibe(Synonyms: PD-132301; ATR-101)

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。

Nevanimibe (Synonyms: PD-132301; ATR-101)

Nevanimibe (PD-132301) 是一种口服有效的,选择性酰基辅酶 A:胆固醇 O-酰基转移酶 1 (ACAT1) 抑制剂,EC50 为 9 nM。Nevanimibe 抑制 ACAT2,EC50 为 368 nM。Nevanimibe 诱导细胞凋亡 (apoptosis),并具有抗肾上腺皮质癌的潜力。

Nevanimibe(Synonyms: PD-132301;  ATR-101)

Nevanimibe Chemical Structure

CAS No. : 133825-80-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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Nevanimibe 的其他形式现货产品:

Nevanimibe hydrochloride

生物活性

Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer[1].

IC50 & Target

ACAT1

9 nM (EC50)

ACAT2

368 nM (EC50)

体外研究
(In Vitro)

Coincubation of Nevanimibe (PD-132301; ATR101; 3 nM-30 μM) and Cholesterol markedly increases toxicity in a dose-dependent manner, where 3 nM Nevanimibe in the presence of 60 μg/mL Cholesterol reduces survival by 60% after 24 hours. All doses of Nevanimibe (3 nM-30 μM) induces cytoxicity in the presence of Cholesterol, whereas treatment with Cholesterol in the absence of Nevanimibe has no effect on cell viability[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 Cytotoxicity Assay[1]

Cell Line: The H295R and HAC clone 15 (HAC15) human ACC cell lines
Concentration: 3 nM-30 μM
Incubation Time: 24 hours
Result: 3 nM-3 μM exhibited no toxicity, whereas 30 μM treatment reduced survival by approximately 40% within 24 hours.

Clinical Trial

分子量

421.62

Formula

C27H39N3O

CAS 号

133825-80-6

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]. LaPensee CR, et al. ATR-101, a Selective and Potent Inhibitor of Acyl-CoA Acyltransferase 1, Induces Apoptosis in H295R Adrenocortical Cells and in the Adrenal Cortex of Dogs. Endocrinology. 2016 May;157(5):1775-88.

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Stuart瓶口药剂分配器PD-P/PD-R/PD-R/HF

【简单介绍】

品牌 其他品牌 产地 进口

英国Stuart瓶口药剂分配器PD-P/PD-R/PD-R/HF,英国进口,为实验室日常的药剂分配器提供一个经济但性能良好的液体分配器选择。为了保证精确性,提供有工业检验证书。 Pressmatic PP是分配许多普通液体的理想工具 包括稀酸,缓冲液,极性溶液和生物学试剂。

【详细说明】

英国Stuart瓶口药剂分配器PD-P/PD-R/PD-R/HF

产品简述:

Pressmatic PP液体分配器, PD-P
特点:
简易的点停式制动环和精确的体积设定
完全支持的带有滴水排檐的分配管 
能完全经受压热器作用
提供单个适配器以适应大多数普通实验室瓶
清除的视界以查看装填过程
精确度< 0.7%
重复性< 0.1%

   Pressmatic PP系列实验室日常的药剂分配器提供一个经济但性能良好的液体分配器选择。为了保证精确性,提供有工业检验证书。 Pressmatic PP是分配许多普通液体的理想工具 包括稀酸,缓冲液,极性溶液和生物学试剂。
由于以聚丙烯阀体、玻璃活塞和分配管,Pressmatic PP不适合用来分配以下的液体:浓酸或者有氧化作用的酸类如浓硫酸,和非极性溶液如烃类、卤代烃等。

Pressmatic R液体分配器, PD-R

主要特点:
全新的人体工程系设计,带有再循环阀
化学防腐性和不粘陶瓷活塞
简单但精确的体积设定
可以完全在瓶口转动,以调整的位置
精确性<0.7%,提供校验证书
可以121°C下对其进行热压处理

Pressmatic分配器有一个创新的设计,能大的增强安全性和使用的简易性。一个在循环阀门意味着用于装填的液体能直接被运回到瓶中,以保证更安全和减少浪费。一旦分配器安装在瓶子上后,它能大程度地转动以调整到好位置。精确的体积设定是通过一个坚固的自动锁定的转动环实现的,使用简单并且在操作过程中不会转动。活塞是高级陶瓷制成的,避免了磨蚀和粘住。液体流动的通道是由玻璃PTFE和陶瓷制成,提供一个出色的防化学腐蚀能力。整台仪器不用拆解就可以对其进行热压处理。每台Pressmatic 分配器提供3个瓶适配器以适用于大部分类型的瓶子和一个工厂校验证书。还有完整系列的备用零件可供使用。

Pressmatic HF液体分配器, PD-R/HF

特点:
全新的人体工程系设计,带有再循环阀
陶瓷/ PTFE液体流管
简易并精确的体积设定
可以完全在瓶口转动,以调整的位置
精确性<0.7%
滴水挑檐

全新的Pressmatic HF分配器特别设计为强腐蚀性的液体如氢弗酸的分配应用。一个再循环阀意味着用于装填的液体能直接被运回到瓶中,以保证更安全和减少浪费。活塞,分配管,阀和, 导管都由化学防腐蚀的陶瓷和PTFE制成。一旦分配器安装在瓶上后,它可以完全在瓶口转动,以调整的位置。精确的体积设定是通过一个坚固的自动锁定的转动环实现的,使用简单并且在操作过程中不会转动。该分配器拆卸简单,很容易清洗,所有的阀门都是可替换的。每台Pressmatic HF分配器提供3个瓶适配器以适用于大部分类型的瓶子和一个工厂校验证书。

英国Stuart瓶口药剂分配器PD-P/PD-R/PD-R/HF

技术指标和订货信息

型号 容量, ml 细分, ml 重复性, % 精确度,%
PD10P 2.0 – 10.0 0.25 <0.1 <0.7
PD60P 10.0 – 60.0 1.00 <0.1 <0.7
PD1R 0.2 – 1.0 0.05 <0.2 <0.7
PD2R 0.4 – 2.0 0.05 <0.1 <0.7
PD5R 1.0 – 5.0 0.10 <0.1 <0.7
PD10R 2.0 – 10.0 0.25 <0.1 <0.1
PD30R 5.0 – 30.0 0.50 <0.1 <0.7
PD60R 10.0 – 60.0 1.00 <0.1 <0.7
PD10R/HF 2.0 – 10.0 0.25 <0.1 <0.7

订货信息

PD10P PP, 2-10ml   
PD10R 2-10ml  
PD10R/HF HF, 2-10ml  
PD1R 0.2-1ml  
PD2R 0.4-2ml  
PD5R 1-5ml
PD10R 2-10ml  
PD30R 5-30ml  
PD60R 10-60ml  

PD-089828

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。

PD-089828 

PD-089828 是 ATP 竞争性 FGFR-1PDGFR-βEGFR (IC50 分别为 0.15, 1.76, 5.47 µM) 抑制剂和 c-Src 酪氨酸激酶非竞争性抑制剂 (IC50=0.18 µM)。PD-089828 也抑制 MAPKIC50 值为 7.1 µM。PD-089828 体外抑制 PDGF-、EGF- 和 bFGF 介导的酪氨酸激酶受体的自磷酸化。PD-089828 具有持久的细胞活性。

PD-089828

PD-089828 Chemical Structure

CAS No. : 179343-17-0

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10 mg ¥5600 询问价格 & 货期

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生物活性

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity[1].

IC50 & Target[1]

FGFR1

0.15 μM (IC50)

PDGFR-β

1.76 μM (IC50)

EGFR

5.47 μM (IC50)

c-Src

0.18 μM (IC50)

FGFR1

0.14 μM (Ki)

PDGFR-β

2.38 μM (Ki)

EGFR

3.16 μM (Ki)

c-Src

0.1 μM (Ki)

体外研究
(In Vitro)

PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC50 of 0.82 µM[1].
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC50 value of 10.9 µM[1].
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC50 value of 0.63 µM[1]. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM[1].
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC50 values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis[1].

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

Cell Proliferation Assay[1]

Cell Line: Vascular smooth muscle cells (serum-stimulated growth)
Concentration: 10 µM
Incubation Time: 8 consecutive days
Result: Produced a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM.

Western Blot Analysis[1]

Cell Line: Vascular smooth muscle cells (stimulated with PDGF-BB 30 ng/ml)
Concentration: 0.5-20 µM
Incubation Time: 2 hours
Result: Inhibited PDGFR autophosphorylation with an IC50 of 0.82 µM.

分子量

405.28

Formula

C18H18Cl2N6O

CAS 号

179343-17-0

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]. Dahring TK, et al. Inhibition of growth factor-mediated tyrosine phosphorylation in vascular smooth muscle by PD 089828, a new synthetic protein tyrosine kinase inhibitor. J Pharmacol Exp Ther. 1997 Jun;281(3):1446-56.

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PD-089828

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。

PD-089828 

PD-089828 是 ATP 竞争性 FGFR-1PDGFR-βEGFR (IC50 分别为 0.15, 1.76, 5.47 µM) 抑制剂和 c-Src 酪氨酸激酶非竞争性抑制剂 (IC50=0.18 µM)。PD-089828 也抑制 MAPKIC50 值为 7.1 µM。PD-089828 体外抑制 PDGF-、EGF- 和 bFGF 介导的酪氨酸激酶受体的自磷酸化。PD-089828 具有持久的细胞活性。

PD-089828

PD-089828 Chemical Structure

CAS No. : 179343-17-0

规格 价格 是否有货
5 mg ¥3300 询问价格 & 货期
10 mg ¥5600 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity[1].

IC50 & Target[1]

FGFR1

0.15 μM (IC50)

PDGFR-β

1.76 μM (IC50)

EGFR

5.47 μM (IC50)

c-Src

0.18 μM (IC50)

FGFR1

0.14 μM (Ki)

PDGFR-β

2.38 μM (Ki)

EGFR

3.16 μM (Ki)

c-Src

0.1 μM (Ki)

体外研究
(In Vitro)

PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC50 of 0.82 µM[1].
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC50 value of 10.9 µM[1].
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC50 value of 0.63 µM[1]. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM[1].
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC50 values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis[1].

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

Cell Proliferation Assay[1]

Cell Line: Vascular smooth muscle cells (serum-stimulated growth)
Concentration: 10 µM
Incubation Time: 8 consecutive days
Result: Produced a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM.

Western Blot Analysis[1]

Cell Line: Vascular smooth muscle cells (stimulated with PDGF-BB 30 ng/ml)
Concentration: 0.5-20 µM
Incubation Time: 2 hours
Result: Inhibited PDGFR autophosphorylation with an IC50 of 0.82 µM.

分子量

405.28

Formula

C18H18Cl2N6O

CAS 号

179343-17-0

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]. Dahring TK, et al. Inhibition of growth factor-mediated tyrosine phosphorylation in vascular smooth muscle by PD 089828, a new synthetic protein tyrosine kinase inhibitor. J Pharmacol Exp Ther. 1997 Jun;281(3):1446-56.

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

WL12

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。

WL12 

WL12 是一种特异性靶向程序性死亡配体 1 (PD-L1) 结合肽。WL12可以通过不同的放射性核素进行放射性标记,产生放射性示踪剂,评估肿瘤 PD-L1 的表达。

WL12

WL12 Chemical Structure

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生物活性

WL12 is a specifically targeting programmed death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled by different radionuclides, generating radiotracers, which can assess the tumor PD-L1 expression[1].

IC50 & Target

PD-L1[1]

分子量

1882.19

Formula

C91H128N22O20S

Sequence Shortening

Cyclo(Ac-Y-{A(Me)}-NPHL-{Hyp}-WS{W(Me)}-{Nle(Me)}-{Nle(Me)}-{Orn}-C)G-NH2 (Thioether bridge: Cys14-Ac-Tyr)

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]. Jiang J, et al. Noninvasive evaluation of PD-L1 expression using Copper 64 labeled peptide WL12 by micro-PET imaging in Chinese hamster ovary cell tumor model. Bioorg Med Chem Lett. 2021 May 15;40:127901.

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

PD0325901-O-C2-dioxolane

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。

PD0325901-O-C2-dioxolane 

PD0325901-O-C2-dioxolane 含有 MEK 抑制剂 PD0325901 主要部分。PD0325901-O-C2-dioxolane 和 VHL 或 CRBN E3 连接酶的配体可用于 MEK1/2 降解剂的合成。

PD0325901-O-C2-dioxolane

PD0325901-O-C2-dioxolane Chemical Structure

CAS No. : 2581116-22-3

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5 mg ¥2200 询问价格 & 货期
10 mg ¥3500 询问价格 & 货期
25 mg ¥7000 询问价格 & 货期
50 mg ¥11500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader[1].

IC50 & Target[1]

MEK1

 

MEK2

 

体外研究
(In Vitro)

PD0325901 is a non-ATP competitive MEK inhibitor, potently inhibits ERK signaling and proliferation of tumor cells[1].

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

分子量

508.23

Formula

C18H16F3IN2O4

CAS 号

2581116-22-3

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]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019;62(23):10897-10911.

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

PD0325901-O-C2-dioxolane

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。

PD0325901-O-C2-dioxolane 

PD0325901-O-C2-dioxolane 含有 MEK 抑制剂 PD0325901 主要部分。PD0325901-O-C2-dioxolane 和 VHL 或 CRBN E3 连接酶的配体可用于 MEK1/2 降解剂的合成。

PD0325901-O-C2-dioxolane

PD0325901-O-C2-dioxolane Chemical Structure

CAS No. : 2581116-22-3

规格 价格 是否有货
5 mg ¥2200 询问价格 & 货期
10 mg ¥3500 询问价格 & 货期
25 mg ¥7000 询问价格 & 货期
50 mg ¥11500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader[1].

IC50 & Target[1]

MEK1

 

MEK2

 

体外研究
(In Vitro)

PD0325901 is a non-ATP competitive MEK inhibitor, potently inhibits ERK signaling and proliferation of tumor 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.

分子量

508.23

Formula

C18H16F3IN2O4

CAS 号

2581116-22-3

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]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019;62(23):10897-10911.

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

PD0325901-O-C2-dioxolane

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。

PD0325901-O-C2-dioxolane 

PD0325901-O-C2-dioxolane 含有 MEK 抑制剂 PD0325901 主要部分。PD0325901-O-C2-dioxolane 和 VHL 或 CRBN E3 连接酶的配体可用于 MEK1/2 降解剂的合成。

PD0325901-O-C2-dioxolane

PD0325901-O-C2-dioxolane Chemical Structure

CAS No. : 2581116-22-3

规格 价格 是否有货
5 mg ¥2200 询问价格 & 货期
10 mg ¥3500 询问价格 & 货期
25 mg ¥7000 询问价格 & 货期
50 mg ¥11500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader[1].

IC50 & Target[1]

MEK1

 

MEK2

 

体外研究
(In Vitro)

PD0325901 is a non-ATP competitive MEK inhibitor, potently inhibits ERK signaling and proliferation of tumor cells[1].

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

分子量

508.23

Formula

C18H16F3IN2O4

CAS 号

2581116-22-3

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]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019;62(23):10897-10911.

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