Acetamide-15N(Synonyms: 乙酰胺 15N)

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。

Acetamide-15N (Synonyms: 乙酰胺 15N)

Acetamide-15N 是 15N 标记的 Acetamide。Acetamide 是合成甲胺,硫代乙酰胺和杀虫剂中间体,也用作皮革,布料和涂料中的增塑剂。 Acetamide 具有致癌性。

Acetamide-15N(Synonyms: 乙酰胺 15N)

Acetamide-15N Chemical Structure

CAS No. : 1449-72-5

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生物活性

Acetamide-15N is the 15N-labeled Acetamide. Acetamide is used as an intermediate in the synthesis of methylamine, thioacetamide, and insecticides, and as a plasticizer in leather, cloth and coatings. Acetamide has carcinogenicity[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

60.06

Formula

C2H515NO

CAS 号

1449-72-5

中文名称

乙酰胺 15N

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]. Acetamide. IARC Monogr Eval Carcinog Risks Hum. 1999;71 Pt 3:1211-21.

    [3]. Moore MM, et, al. The food contaminant acetamide is not an in vivo clastogen, aneugen, or mutagen in rodent hematopoietic tissue. Regul Toxicol Pharmacol. 2019 Nov;108:104451.

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Duocarmycin GA(Synonyms: 倍癌霉素 GA)

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。

Duocarmycin GA (Synonyms: 倍癌霉素 GA)

Duocarmycin GA 是抗体偶联药物 (ADCs) 中的毒素分子。Duocarmycin 是一种 DNA 烷化剂,靶向 DNA 小沟。Duocarmycin GA 可用于抗多药耐药细胞系。

Duocarmycin GA(Synonyms: 倍癌霉素 GA)

Duocarmycin GA Chemical Structure

CAS No. : 1613286-59-1

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生物活性

Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.

IC50 & Target

Duocarmycins

 

分子量

476.95

Formula

C26H25ClN4O3

CAS 号

1613286-59-1

中文名称

倍癌霉素 GA

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]. Searcey M. Duocarmycins–natures prodrugs? Curr Pharm Des. 2002;8(15):1375-89.

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c-Met-IN-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。

c-Met-IN-1 

c-met-IN-1 (compound 16) 是一种高效选择性的 c-Met 抑制剂,IC50 值为 1.1 nM,具有抗肿瘤活性。

c-Met-IN-1

c-Met-IN-1 Chemical Structure

CAS No. : 2084836-84-8

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生物活性

c-met-IN-1 (compound 16) is a potent and selective c-Met inhibitor, with IC50 of 1.1 nM, with antitumor activity.[1].

IC50 & Target

IC50: 1.1 nM (c-Met)[1]

体外研究
(In Vitro)

c-met-IN-1 (compound 16) exhibits high selectivity and remarkable cytotoxicity against HT-29, MKN-45 and A549 cells with IC50 values of 0.08 μM, 0.22 μM and 0.07 μM, respectively[1].

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

分子量

640.70

Formula

C35H37FN6O5

CAS 号

2084836-84-8

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]. Wang X, et al. Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors. Bioorg Med Chem. 2017 Feb 1;25(3):886-896.

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MS4077

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。

MS4077  纯度: 99.49%

MS4077 是基于 Cereblon 配体的间变性淋巴瘤激酶 (ALK) PROTAC (降解物),结合 ALK, Kd 为 37 nM。

MS4077

MS4077 Chemical Structure

CAS No. : 2230077-10-6

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1 mg ¥3500 In-stock
5 mg ¥10500 In-stock
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MS4077 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 37 nM for binding affinity to ALK[1].

IC50 & Target

ALK

 

Cereblon

 

体外研究
(In Vitro)

MS4077 effectively inhibits cancer cell proliferation. MS4077 (10-3-1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC50 of 46 ± 4 nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4077(10-2-100.5 μM; 3 days)[1].
MS4077 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In SU-DHL-1 cells, MS4077 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of 3±1 nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100 nM concentration. In NCI-H2228 cells, MS4077 reduces the EML4-ALK protein levels with similar DC50 value of 34±9 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels[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: SU-DHL-1 and NCI-H2228 cells
Concentration: 10-3, 10-2.5, 10-2,10-1.5, 10-1, 10-0.5, and 1 μM for SU-DHL-1  cells; 10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM for NCI-H2228 cells
Incubation Time: 3 days
Result: Inhibited proliferation of SU-DHL-1 cells (IC50=46 ± 4 nM). Less sensitive to the proliferation of NCI-H2228 cells than SU-DHL-1 cells.

Western Blot Analysis[1]

Cell Line: SU-DHL-1 and NCI-H2228 cells
Concentration: 1, 3, 10, 30, and 100 μM for SU-DHL-1 cells; 3, 10, 30, 60, and 100 μM for NCI-H2228 cells
Incubation Time: 16 hours
Result: Reduced the NPM-ALK protein levels with impressive DC50 of  3 ± 1 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC50 of 34 ± 9 nM in NCI-H2228 cells.

分子量

1134.73

Formula

C55H72ClN9O13S

CAS 号

2230077-10-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 110 mg/mL (96.94 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8813 mL 4.4063 mL 8.8127 mL
5 mM 0.1763 mL 0.8813 mL 1.7625 mL
10 mM 0.0881 mL 0.4406 mL 0.8813 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 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

    此方案可获得 6 mg/mL (5.29 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 60.0 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 mg/mL (5.29 mM); Clear solution

    此方案可获得 ≥ 6 mg/mL (5.29 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 60.0 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
*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]. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.

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AMG 925

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。

AMG 925  纯度: 98.24%

AMG 925 是一种有效的选择性的 FLT3/CDK4 双重抑制剂,IC50 分别为 2±1 nM 和 3±1 nM。

AMG 925

AMG 925 Chemical Structure

CAS No. : 1401033-86-0

规格 价格 是否有货 数量
5 mg ¥850 In-stock
10 mg ¥1200 In-stock
50 mg ¥3500 In-stock
100 mg ¥5500 In-stock
200 mg   询价  
500 mg   询价  

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AMG 925 相关产品

相关化合物库:

  • Bioactive Compound Library Plus

生物活性

AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.

IC50 & Target[1]

FLT3

2 nM (IC50)

CDK4

3 nM (IC50)

CDK6

8 nM (IC50)

CDK2

375 nM (IC50)

CDK1

1.9 μM (IC50)

体外研究
(In Vitro)

AMG 925 also inhibits CDK6, CDK2, and CDK1 in kinase assays with IC50s of 8±2 nM, 375±150 nM, 1.90±0.51 μM, respectively. A fair overall kinase selectivity of AMG 925 is as determined by KinomScan against a panel of 442 various kinases. Cellular selectivity (on-target vs. off-target activity) of AMG 925 is about 50-fold as evaluated by comparison of its growth-inhibiting activity in RB-positive (RB+) and RB-negative (RB) non- acute myeloid leukemia (AML) cancer cell lines. AMG 925 potently inhibits growth of AML cell lines MOLM13 (FLT3-ITD; IC50=19 μM) and Mv4-11 (FLT3-ITD; IC50=18 μM)[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)

MOLM13 tumor-bearing mice are dosed twice daily by oral administration 6 hours apart with 12.5, 25, or 37.5 mg/kg AMG 925. Tumors are then harvested 3, 9, 12, and 24 hours after the first dose, and analyzed for levels of P-STAT5 and P-RB. Maximum inhibition of P-STAT5 and P-RB is achieved at 6 and 12 hours respectively at the 37.5 mg/kg dose of AMG 925. Interestingly, a rebound of P-STAT5 at 24 hours is observed, possibly as a result of compensational feedback. The pharmacodynamic responses of P-STAT5 and P-RB inhibition correlated with plasma concentrations of AMG 925. AMG 925 inhibits AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlates with the inhibition of STAT5 and retinoblastoma protein (RB) phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 is also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and Sorafenib)[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

471.55

Formula

C26H29N7O2

CAS 号

1401033-86-0

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: 

H2O : < 0.1 mg/mL (insoluble)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

参考文献
  • [1]. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

Cell Assay
[1]

MOLM13 and Mv4-11 are used. MOLM13-Luc cells are constructed by transduction of MOLM13 cells with the pLV218G luciferin/lentivector, which expresses luciferase under the murine EF1α promoter. Sorafenib-resistant MOLM13 (MOLM13sr) and Mv4-11 (Mv4-11sr) are isolated by passaging the cells in growth medium containing increasing concentrations of Sorafenib (1-1 nM). Cell growth is measured by a DNA synthesis assay. Cells are seeded in a 96-well Cytostar T plate at a density of 5×103 cells/well in a total volume of 160 μL. Test compounds (e.g., AMG 925; 0.03 and 0.3μM) are serially diluted into the plate (20 μL/well) and 20 μL/0.1 μCi of [14C]-Thymidine added to each well. Isotope incorporation is determined using a β plate counter after further 72-hour incubation. Apoptosis is assayed by using the Vybrant Apoptosis Assay Kit. Briefly, cells are seeded into a 6-well plate at 5×105 cells per well and treated with compounds (e.g., AMG 925; 0.003, 0.01, 0.03, 0.1, 0.3, and 1 μM) for 24 hours. The cells are then stained with reagents provided in the kit and analyzed by flow cytometry. The Sytox Green fluorescence versus allophycocyanin fluorescence dot plot shows resolution of live, apoptotic, and dead cells, which are quantified using the Flowjo software. The cell-cycle analysis is done by treating the cells with AMG 925 for 24 hours followed by using the CycleTest Kit. Ten thousand events are acquired and the proportions of cells in each cycle phase are calculated using the ModFit software[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 Administration
[1]

Mice[1]
CrTac:NCR-Foxn1nu (NCR) nude mice are used. 2×106 cells are innoculated on the flank of NCR nude mice and allowed to grow for 13 days. Mice are then dosed twice a day by oral administration 6 hours apart with 12.5, 25, 37.5, and 50 mg/kg of AMG 925 for 10 consecutive days[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.

参考文献
  • [1]. Keegan K, et al. Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.

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不锈钢标准系列砝码 单只毫克系列 20mg E2

不锈钢标准系列砝码 单只毫克系列 20mg E2

不锈钢标准系列砝码 单只毫克系列 20mg E2

  • 商品品牌: 富月
    商品编号: 20mg E2
  • 商品价格: 请与我们联系
  • 不锈钢标准系列砝码 单只毫克系列 20mg E2-富月-20mg E2

    • 产品类型:单个砝码
    • 砝码等级:E2
    • 产品规格: 单只毫克系列 20mg
    • 材质:无磁不锈钢
    实验室常用设备|||天平、泵|||砝码|||不锈钢标准系列砝码单只毫克系列20mgE2
    不锈钢/单个/砝码组合/砝码
    不锈钢标准系列砝码 单只毫克系列 20mg E2

    材质:无磁不锈钢

    等级:E2、F1

    密度:7.94-7.96g/cm³

    包装:环保铝盒、塑料盒

    内衬:国产环保泡棉

    商品属性

    • 产品类型:单个砝码
    • 砝码等级:E2
    • 产品规格: 单只毫克系列 20mg
    • 材质:无磁不锈钢
    商品属性
    商品名称 不锈钢标准系列砝码 单只毫克系列 20mg E2-20mg E2-富月
    型号 20mg E2
    类别 实验室常用设备|||天平、泵|||砝码|||不锈钢标准系列砝码单只毫克系列20mgE2
    品牌 富月
    品牌简介 富月
    关键字 不锈钢/单个/砝码组合/砝码,砝码,不锈钢,系列,标准,组合,内衬

    不锈钢标准系列砝码 单只毫克系列 20mg E2

    ML327

    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。

    ML327  纯度: 98.19%

    ML327 是 MYC 的阻断剂,也可以去阻遏 E-钙粘蛋白转录和逆转上皮-间质转化 (EMT)。

    ML327

    ML327 Chemical Structure

    CAS No. : 1883510-31-3

    规格 价格 是否有货 数量
    10 mM * 1 mL in DMSO ¥5720 In-stock
    1 mg ¥1500 In-stock
    5 mg ¥5200 In-stock
    10 mg ¥8200 In-stock
    25 mg ¥15000 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    ML327 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Apoptosis Compound Library
    • Anti-Cancer Compound Library
    • Autophagy Compound Library
    • Glutamine Metabolism Compound Library
    • Transcription Factor Targeted Library
    • Targeted Diversity Library

    生物活性

    ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).

    IC50 & Target

    MYC[1]

    体外研究
    (In Vitro)

    Treatment with ML327 induces an elongated morphology in neuroblastoma cells. BE(2)-C cells treated with ML327 demonstrates G1 cell cycle arrest with a concordant decrease in S phase population, and a significant increase in the sub G0 population. ML327 induces the expression of CDH1 in all seven of the neuroblastoma cell lines with a 50 to 1,400-fold induction of CDH1 mRNA expression. ML327 blocks the expression of MYC family of oncogenic transcription factors in all tested neuroblastoma cell lines. Immunoblotting time course demonstrates early repression of N-MYC expression within 2 h of treatment with ML327 (10 µM). p53 levels are also suppressed by treatment with ML327. ML327-pretreated cells demonstrates reduced proliferative potential in both tetrazolium-based (p<0.0001) and adherent 2D colony formation (41 vs. 400; p<0.0001)[1]. ML327 reduces SW620inv cell invasion through Matrigel by ~60% and reduces H520 cell invasion by ~30% in these in vitro assays. ML327 partially restores E-cadherin expression at the plasma membrane in NMuMG cells induced to undergo Epithelial-to-Mesenchymal Transition (EMT) by TGF-β1 treatment[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)

    ML327 treatment significantly reduces tumor volume by three-fold over the two-week treatment period (p=0.02). Tumor explant weights are approximately three-fold smaller in the ML327-treated mice (p=0.01). Mice treated with ML327 lost 12% more body weight than vehicle treated mice. ML327 treatment results in a two-fold decrease in MYCN expression, confirming that ML327 inhibits xenograft MYCN expression (p=0.0035)[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

    366.37

    Formula

    C19H18N4O4

    CAS 号

    1883510-31-3

    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 : 32 mg/mL (87.34 mM; Need ultrasonic and warming)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7295 mL 13.6474 mL 27.2948 mL
    5 mM 0.5459 mL 2.7295 mL 5.4590 mL
    10 mM 0.2729 mL 1.3647 mL 2.7295 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]. Rellinger EJ, et al. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Jul 20;8(53):91040-91051.

      [2]. An H, et al. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.Oncotarget. 2015 Sep 8;6(26):22934-48.

    Cell Assay
    [1]

    Cells are seeded onto 96-well plates at equivalent density (3,000 to 10,000 depending upon cell line), permitted to attach overnight, and treated with either ML327 (10 μM) or vehicle. Daily absorbance measurements (450 nm) using the cell counting kit are obtained. For estimation of IC50 values, cells are plated at equal density, permitted to attach, and baseline absorbance is obtained using cell counting kit. Cells are then treated with varying doses of ML327 (0.1 to 30 μM) and cell viability is measured 72 h after treatment[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 Administration
    [1]

    Male athymic nude mice (4 to 6 weeks old) are maintained as described. BE(2)-C cells xenografts are established as previously described. Briefly, 1×106 cells/100 µL of HBSS are injected subcutaneously into flanks using a 26-gauge needle (n=10 per group). Mice are monitored daily for xenograft formation and assessed by measuring the two greatest perpendicular tumor diameter with venier calipers. Xenograft volumes are estimated using the following formula [(length×width2)/2]. Once tumors reach 75 to 100 mm3, mice are randomized to receive either 50 mg/kg of ML327 or control vehicle (70% polyethylene glycol) via intraperitoneal injection twice daily for 14d. Weight and tumor volume are recorded daily. After completion of two weeks of treatment, mice are euthanized and tumors are excised, weighed, and RNA is isolated[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.

    参考文献
    • [1]. Rellinger EJ, et al. Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma. Oncotarget. 2017 Jul 20;8(53):91040-91051.

      [2]. An H, et al. Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.Oncotarget. 2015 Sep 8;6(26):22934-48.

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    Estriol-d2(Synonyms: 雌三醇 d2)

    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。

    Estriol-d2 (Synonyms: 雌三醇 d2)

    Estriol-d2 是 Estriol 的氘代物。Estriol是G蛋白偶联雌激素受体拮抗剂,可作用于雌激素受体阴性乳腺癌细胞。

    Estriol-d2(Synonyms: 雌三醇 d2)

    Estriol-d2 Chemical Structure

    CAS No. : 53866-32-3

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

    * Please select Quantity before adding items.

    生物活性

    Estriol-d2 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

    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

    290.39

    Formula

    C18H22D2O3

    CAS 号

    53866-32-3

    中文名称

    雌三醇 d2

    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]. Morinaga, A., et al., Effects of sex hormones on Alzheimer’s disease-associated beta-amyloid oligomer formation in vitro. Exp Neurol, 2011. 228(2): p. 298-302.

      [3]. Begum, M., et al., Neonatal estrogenic exposure suppresses PTEN-related endometrial carcinogenesis in recombinant mice. Lab Invest, 2006. 86(3): p. 286-96.

      [4]. Hewitt, S.C. and K.S. Korach, Estrogenic activity of bisphenol A and 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) demonstrated in mouse uterine gene profiles. Environ Health Perspect, 2011. 119(1): p. 63-70.

    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

    LCL521

    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。

    LCL521 

    LCL521 是一种酸性神经酰胺酶 (ACDase) 抑制剂。LCL521 还抑制溶酶体酸性鞘磷脂酶 (ASMase)。

    LCL521

    LCL521 Chemical Structure

    CAS No. : 1226851-11-1

    规格 价格 是否有货
    10 mM * 1 mL in DMSO ¥4564 询问价格 & 货期
    5 mg ¥3500 询问价格 & 货期
    10 mg ¥5500 询问价格 & 货期
    50 mg ¥16500 询问价格 & 货期
    100 mg ¥26500 询问价格 & 货期

    * Please select Quantity before adding items.

    LCL521 的其他形式现货产品:

    LCL521 dihydrochloride

    LCL521 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Metabolism/Protease Compound Library
    • Anti-Cancer Compound Library
    • Lipid Metabolism Compound Library

    生物活性

    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase)[1].

    IC50 & Target

    ACDase, ASMase[1]

    体外研究
    (In Vitro)

    LCL521 (1 µM) acts as a potent inhibitor of cellular ACDase activity, whereas 10 µM LCL521 has an additional, decreased affect on the α-form of this enzyme. LCL521 (10 µM) causes a time-dependent (1 hours and 5 hours) decrease of the α-ACDase form in MCF7 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

    592.77

    Formula

    C31H52N4O7

    CAS 号

    1226851-11-1

    运输条件

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 165 mg/mL (278.35 mM; Need ultrasonic)

    Ethanol : 100 mg/mL (168.70 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.6870 mL 8.4350 mL 16.8699 mL
    5 mM 0.3374 mL 1.6870 mL 3.3740 mL
    10 mM 0.1687 mL 0.8435 mL 1.6870 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 (4.64 mM); Clear solution

      此方案可获得 ≥ 2.75 mg/mL (4.64 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 (4.64 mM); Clear solution

      此方案可获得 ≥ 2.75 mg/mL (4.64 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 (4.64 mM); Clear solution

      此方案可获得 ≥ 2.75 mg/mL (4.64 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]. Bai A, et al. Targeting (cellular) lysosomal acid ceramidase by B13: design, synthesis and evaluation of novel DMG-B13 ester prodrugs. Bioorg Med Chem. 2014 Dec 15;22(24):6933-44.

    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

    BI-4464

    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。

    BI-4464  纯度: 99.27%

    BI-4464 是具有高度选择性的,ATP竞争性的、PTK2/FAK 的抑制剂,其IC50 值为 17 nM。是可用于PROTAC 降解剂的一个PTK2 配体。

    BI-4464

    BI-4464 Chemical Structure

    CAS No. : 1227948-02-8

    规格 价格 是否有货 数量
    5 mg ¥3700 In-stock
    10 mg ¥5950 In-stock
    50 mg 询价
    100 mg 询价

    * Please select Quantity before adding items.

    BI-4464 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus

    生物活性

    BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC[1].

    IC50 & Target

    IC50: 17 nM (PTK2/FAK)[1].

    分子量

    555.55

    Formula

    C28H28F3N5O4

    CAS 号

    1227948-02-8

    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 : 16.67 mg/mL (30.01 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8000 mL 9.0001 mL 18.0002 mL
    5 mM 0.3600 mL 1.8000 mL 3.6000 mL
    10 mM 0.1800 mL 0.9000 mL 1.8000 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]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520.

    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

    CDK7-IN-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。

    CDK7-IN-1  纯度: 98.91%

    CDK7-IN-1,是YKL-5-124 的类似物,是一种细胞周期蛋白依赖性激酶 7 (cdk7) 抑制剂,IC50 值小于 100 nM,来自专利 WO 2016105528 A2 化合物实例 215。

    CDK7-IN-1

    CDK7-IN-1 Chemical Structure

    CAS No. : 1957203-02-9

    规格 价格 是否有货 数量
    1 mg ¥1900 In-stock
    5 mg ¥5900 询价
    10 mg ¥9900 询价
    25 mg ¥19900 询价
    50 mg ¥29900 询价
    100 mg   询价  
    200 mg   询价  

    * Please select Quantity before adding items.

    生物活性

    CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215[1].

    IC50 & Target[1]

    CDK7

    100 nM (IC50)

    分子量

    517.62

    Formula

    C28H35N7O3

    CAS 号

    1957203-02-9

    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
    参考文献
    • [1]. Nathanael S. Gray, et al Inhibitors of cyclin-dependent kinase 7 (cdk7). WO 2016105528 A2

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    MT1

    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。

    MT1  纯度: 98.37%

    MT1 是 BET bromodomains 的化学探针,其对BRD4(1) 的 IC50 值为 0.789 nM。

    MT1

    MT1 Chemical Structure

    CAS No. : 2060573-82-0

    规格 价格 是否有货 数量
    1 mg ¥2500 In-stock
    5 mg ¥6500 In-stock
    10 mg ¥10500 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    MT1 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus

    生物活性

    MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1)[1].

    体外研究
    (In Vitro)

    MT1 (100 nM, 24 h) significantly induces apoptosis via caspase-3 and PARP in MV4;11 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.

    Western Blot Analysis[1]

    Cell Line: MV4;11 cells[1].
    Concentration: 100 nM.
    Incubation Time: 24 h.
    Result: Significant apoptosis was observed by caspase-3 and PARP cleavage after treatment.

    体内研究
    (In Vivo)

    MT1 (44.2 and 22.1 µmol/kg, ip daily, for 14 days) significantly delayed leukemia progression in mice (Mus musculus) compared to JQ1[1].
    MT1 exhibits terminal t1/2 of 2.70 h in 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: Leukemia xenograft models[1].
    Dosage: 44.2 and 22.1 µmol/kg.
    Administration: Intraperitoneally for 14 subsequent days.
    Result: Significantly reduced leukemic burden over the course of the study compared to either vehicle or JQ1.

    分子量

    1134.20

    Formula

    C54H66Cl2N10O9S2

    CAS 号

    2060573-82-0

    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 : 150 mg/mL (132.25 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 0.8817 mL 4.4084 mL 8.8168 mL
    5 mM 0.1763 mL 0.8817 mL 1.7634 mL
    10 mM 0.0882 mL 0.4408 mL 0.8817 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: ≥ 7.5 mg/mL (6.61 mM); Clear solution

      此方案可获得 ≥ 7.5 mg/mL (6.61 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 75.0 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: 7.5 mg/mL (6.61 mM); Suspended solution; Need ultrasonic

      此方案可获得 7.5 mg/mL (6.61 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 75.0 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: ≥ 7.5 mg/mL (6.61 mM); Clear solution

      此方案可获得 ≥ 7.5 mg/mL (6.61 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 75.0 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]. Minoru Tanaka, et al. Design and characterization of bivalent BET inhibitors. Nat Chem Biol. 2016 Dec;12(12):1089-1096.

    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

    G280-9

    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。

    G280-9 

    G280-9 是含有 9 个氨基酸的天然表位肽。G280-9 是在黑素瘤上表达的相关靶蛋白。

    G280-9

    G280-9 Chemical Structure

    CAS No. : 156761-76-1

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

    * Please select Quantity before adding items.

    生物活性

    G280-9 is a 9 amino acid native epitope peptide. G280-9 is a relevant target expressed on melanoma.

    分子量

    946.05

    Formula

    C44H67N9O14

    CAS 号

    156761-76-1

    Sequence

    Tyr-Leu-Glu-Pro-Gly-Pro-Val-Thr-Ala

    Sequence Shortening

    YLEPGPVTA

    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.

    Solvent & Solubility
    In Vitro: 

    H2O

    Peptide Solubility and Storage Guidelines:

    1.  Calculate the length of the peptide.

    2.  Calculate the overall charge of the entire peptide according to the following table:

      Contents Assign value
    Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
    Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
    Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

    3.  Recommended solution:

    Overall charge of peptide Details
    Negative (<0) 1.  Try to dissolve the peptide in water first.
    2.  If water fails, add NH4OH (<50 μL).
    3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
    Positive (>0) 1.  Try to dissolve the peptide in water first.
    2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
    3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
    Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
    2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
    参考文献
    • [1]. Pass HA, et al. Immunization of patients with melanoma peptide vaccines: immunologic assessment using the ELISPOT assay. Cancer J Sci Am. 1998 Sep-Oct;4(5):316-23.

    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

    DTP3

    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。

    DTP3  纯度: 99.43%

    DTP3 TFA 是一种有效的选择性 GADD45β/MKK7 抑制剂。DTP3 TFA 靶向 NF-κB 通路下游,具有抗癌活性。

    DTP3

    DTP3 Chemical Structure

    CAS No. : 1809784-29-9

    规格 价格 是否有货 数量
    Free Sample (0.1-0.5 mg)   Apply now  
    5 mg ¥1600 In-stock
    10 mg ¥2800 In-stock
    25 mg ¥4000 In-stock
    50 mg ¥5500 In-stock
    100 mg ¥8000 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    DTP3 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Cell Cycle/DNA Damage Compound Library
    • Epigenetics Compound Library
    • Immunology/Inflammation Compound Library
    • JAK/STAT Compound Library
    • Kinase Inhibitor Library
    • NF-κB Signaling Compound Library
    • Stem Cell Signaling Compound Library
    • Anti-Cancer Compound Library
    • Anti-Aging Compound Library
    • Differentiation Inducing Compound Library
    • Reprogramming Compound Library
    • Anti-Breast Cancer Compound Library
    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Anti-Blood Cancer Compound Library
    • Targeted Diversity Library
    • Anti-Liver Cancer Compound Library

    生物活性

    DTP3 TFA is a potent and selective GADD45β/MKK7 inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway[1].

    体外研究
    (In Vitro)

    DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours[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)

    DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice[2].
    DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg[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.

    Animal Model: 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2]
    Dosage: 14.5 mg/kg
    Administration: S.c.; daily; 28 days
    Result: Had shown a dramatic shrinkage of the tumors.
    Animal Model: CD1 male mice of 25-30 g[2]
    Dosage: 10 mg/kg (Pharmacokinetic Study)
    Administration: Intravenous injection
    Result: Had t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg.

    分子量

    525.60

    Formula

    C26H35N7O5

    CAS 号

    1809784-29-9

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Protect from light

    Powder -80°C 2 years
    -20°C 1 year

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

    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (190.26 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9026 mL 9.5129 mL 19.0259 mL
    5 mM 0.3805 mL 1.9026 mL 3.8052 mL
    10 mM 0.1903 mL 0.9513 mL 1.9026 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: ≥ 2.5 mg/mL (4.76 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.76 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% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.76 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 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 (4.76 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.76 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]. Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.

      [2]. Tornatore L, et al. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508.

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    Peptide C105Y

    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。

    Peptide C105Y 

    Peptide C105Y,基于 α1-抗胰蛋白酶 359-374 残基氨基酸序列合成的细胞穿透性肽,能增强 DNA 纳米粒的基因表达。

    Peptide C105Y

    Peptide C105Y Chemical Structure

    CAS No. : 247572-63-0

    规格 价格 是否有货
    5 mg ¥4000 询问价格 & 货期
    10 mg ¥6800 询问价格 & 货期

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    生物活性

    Peptide C105Y, a synthetic and cell-penetrating peptide based on the amino acid sequence corresponding to residues 359-374 of α1-antitrypsin, enhances gene expression from DNA nanoparticles[1].

    体外研究
    (In Vitro)

    When human hepatoma cells (HuH7) were incubated with fluorescently labeled C105Y for as little as 3 min, C105Y displays nuclear and cytoplasmic staining with enrichment of fluorescent signal in the nucleus and nucleolus. C105Y peptide is routed to the nucleolus very rapidly in an energy-dependent fashion, whereas membrane translocation and nuclear localization are energy-independent. When tested the involvement of known endocytosis pathways in uptake and trafficking of this peptide, C105Y peptide is internalized by a clathrin- and caveolin-independent pathway, although lipid raft-mediated endocytosis may play a role in peptide intracellular trafficking[1].

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

    分子量

    1994.40

    Formula

    C97H148N20O23S

    CAS 号

    247572-63-0

    Sequence

    Cys-Ser-Ile-Pro-Pro-Glu-Val-Lys-Phe-Asn-Lys-Pro-Phe-Val-Tyr-Leu-Ile

    Sequence Shortening

    CSIPPEVKFNKPFVYLI

    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]. Rhee M, et al. Mechanism of uptake of C105Y, a novel cell-penetrating peptide. J Biol Chem. 2006 Jan 13;281(2):1233-40.

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    FAPI-2

    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。

    FAPI-2 

    FAPI-2 是一种成纤维细胞活化蛋白 (FAP) 抑制剂,可用于癌症研究。

    FAPI-2

    FAPI-2 Chemical Structure

    CAS No. : 2370952-98-8

    规格 是否有货
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    500 mg   询价  

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    生物活性

    FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research[1].

    IC50 & Target

    Fibroblast activation protein (FAP)[1]

    分子量

    836.93

    Formula

    C40H56N10O10

    CAS 号

    2370952-98-8

    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]. Giesel FL, et al. 68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers. J Nucl Med. 2019 Mar;60(3):386-392.

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    Pep-1 (uncapped)

    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。

    Pep-1 (uncapped) 

    Pep-1 (uncapped) 是一种可透过细胞的多肽。

    Pep-1 (uncapped)

    Pep-1 (uncapped) Chemical Structure

    CAS No. : 395069-86-0

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

    * Please select Quantity before adding items.

    生物活性

    Pep-1 (uncapped) is a cell-penetrating peptide.

    分子量

    2848.22

    Formula

    C136H195N35O33

    CAS 号

    395069-86-0

    Sequence

    Lys-Glu-Thr-Trp-Trp-Glu-Thr-Trp-Trp-Thr-Glu-Trp-Ser-Gln-Pro-Lys-Lys-Lys-Arg-Lys-Val

    Sequence Shortening

    KETWWETWWTEWSQPKKKRKV

    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.

    Solvent & Solubility
    In Vitro: 

    H2O

    Peptide Solubility and Storage Guidelines:

    1.  Calculate the length of the peptide.

    2.  Calculate the overall charge of the entire peptide according to the following table:

      Contents Assign value
    Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
    Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
    Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

    3.  Recommended solution:

    Overall charge of peptide Details
    Negative (<0) 1.  Try to dissolve the peptide in water first.
    2.  If water fails, add NH4OH (<50 μL).
    3.  If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
    Positive (>0) 1.  Try to dissolve the peptide in water first.
    2.  If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
    3.  If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
    Zero (=0) 1.  Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
    2.  For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
    参考文献
    • [1]. Almarwani B, et al. Vesicles mimicking normal and cancer cell membranes exhibit differential responses to the cell-penetrating peptide Pep-1. Biochim Biophys Acta Biomembr. 2018 Jun;1860(6):1394-1402.

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    5-IAF(Synonyms: 5-碘乙酰氨基荧光素; 5-Iodoacetamidofluorescein)

    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。

    5-IAF (Synonyms: 5-碘乙酰氨基荧光素; 5-Iodoacetamidofluorescein) 纯度: ≥95.0%

    5-IAF 是荧光素的偶氮乙酰胺衍生物。

    5-IAF(Synonyms: 5-碘乙酰氨基荧光素; 5-Iodoacetamidofluorescein)

    5-IAF Chemical Structure

    CAS No. : 63368-54-7

    规格 价格 是否有货 数量
    5 mg ¥770 In-stock
    10 mg   询价  
    50 mg   询价  

    * Please select Quantity before adding items.

    5-IAF 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Anti-Cancer Compound Library

    生物活性

    5-IAF is an idoacetamide derivate of fluoresceine.

    体外研究
    (In Vitro)

    8 µM GSH sample solution is derivatized with 8, 80, 200, 400, 800, 1600, 2000, 2500 µM 5-IAF, respectively and analyzed with CE-LIF. The highest signal intensity is obtained with 400 and 800 µM 5-IAF[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.

    分子量

    515.25

    Formula

    C22H14INO6

    CAS 号

    63368-54-7

    中文名称

    5-碘乙酰氨基荧光素

    运输条件

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 50 mg/mL (97.04 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9408 mL 9.7040 mL 19.4081 mL
    5 mM 0.3882 mL 1.9408 mL 3.8816 mL
    10 mM 0.1941 mL 0.9704 mL 1.9408 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: 1.43 mg/mL (2.78 mM); Suspended solution; Need ultrasonic

      此方案可获得 1.43 mg/mL (2.78 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 14.3 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: 1.43 mg/mL (2.78 mM); Suspended solution; Need ultrasonic

      此方案可获得 1.43 mg/mL (2.78 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 14.3 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
    *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]. Salvatore Sotgia, et al. Plasma L-Ergothioneine Measurement by High-Performance Liquid Chromatography and Capillary Electrophoresis after a Pre-Column Derivatization with 5-Iodoacetamidofluorescein (5-IAF) and Fluorescence Detection. PLoS One. 2013; 8(7): e70374.

      [2]. Yan Wang, et al. Determination of free and protein-bound glutathione in HepG2 cells using capillary electrophoresis with laser-induced fluorescence detection. J Chromatogr A. 2009 Apr 17;1216(16):3533-7.

    Kinase Assay
    [2]

    HepG2 cells are lysed in 1 mL 2% acetonitrile in water, and transfered to a 1.5 mL centrifuge tube. An additional 200 µL 2% acetonitrile is used to rinse the dish and combined with the cell extract. To measure the free GSH concentration, three aliquots of 80 µL cell extract are immediately transferred to 0.5 mL centrifuge tubes after a quick mix. Then 20 µL 50 µM NAC is added, followed by the addition of 100 µL 400 µM 5-IAF to the mixture. The derivatization is conducted at room temperature in dark for 1 h, after which the mixtures are centrifuged at 9000× g for 5 min to sediment the insoluble proteins. 10 µL supernatant is diluted 100× with water and analyzed immediately by CE-LIF[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.

    参考文献
    • [1]. Salvatore Sotgia, et al. Plasma L-Ergothioneine Measurement by High-Performance Liquid Chromatography and Capillary Electrophoresis after a Pre-Column Derivatization with 5-Iodoacetamidofluorescein (5-IAF) and Fluorescence Detection. PLoS One. 2013; 8(7): e70374.

      [2]. Yan Wang, et al. Determination of free and protein-bound glutathione in HepG2 cells using capillary electrophoresis with laser-induced fluorescence detection. J Chromatogr A. 2009 Apr 17;1216(16):3533-7.

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    NLS (PKKKRKV)

    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。

    NLS (PKKKRKV) 

    NLS (PKKKRKV) 是一种源于 SV40 large T antigen 的 NLS,可作为增强核进入方法应用于基因导入。

    NLS (PKKKRKV)

    NLS (PKKKRKV) Chemical Structure

    CAS No. : 95088-49-6

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    NLS (PKKKRKV) 的其他形式现货产品:

    NLS (PKKKRKV) (hydrochloride)

    生物活性

    NLS (PKKKRKV) is a nuclear localization signal (NLS) derived from the simian virus 40 large tumor antigen (SV40 large T antigen). NLS (PKKKRKV) can function as a method to enhance nuclear entry in the field of gene transfer research[1][2].

    分子量

    883.14

    Formula

    C40H78N14O8

    CAS 号

    95088-49-6

    Sequence Shortening

    PKKKRKV

    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]. Zanta MA, et al. Gene delivery: A single nuclear localization signal peptide is sufficient to carry DNA to the cell nucleus. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):91-6.

      [2]. Cao S, et al. Enhanced effect of nuclear localization signal peptide during ultrasound-targeted microbubble destruction-mediated gene transfection. Mol Med Rep. 2017 Jul;16(1):565-572.

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    G3-C12 TFA

    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。

    G3-C12 TFA  纯度: 99.45%

    G3-C12 (TFA) 是 galectin-3 结合肽,Kd 值为 88 nM,具有抗肿瘤活性。

    G3-C12 TFA

    G3-C12 TFA Chemical Structure

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    G3-C12 TFA 相关产品

    相关化合物库:

    • Bioactive Compound Library Plus
    • Peptide Library

    生物活性

    G3-C12 (TFA) is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.

    IC50 & Target

    Kd: 88 nM (Galectin-3)[1].

    体外研究
    (In Vitro)

    G3-C12 (TFA) is a galectin-3 binding peptide, with high affinity (Kd) of 88 nM, but shows no affinity for other galectin family members or to other lectins. G3-C12 (TFA) bearing opolymers N-(2-hydroxypropyl)methacrylamide (HPMA) potently and selectively targets colorectal cancer (CRC) tumour cells over-expressing galectin-3 and displays superior targetability to galectin-3 compared to the galactose bearing copolymer[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

    1873.00

    Formula

    C74H115N23O23S2.C2HF3O2

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Sealed storage, away from moisture

    Powder -80°C 2 years
    -20°C 1 year

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

    溶解性数据
    In Vitro: 

    H2O : ≥ 50 mg/mL (26.70 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 0.5339 mL 2.6695 mL 5.3390 mL
    5 mM 0.1068 mL 0.5339 mL 1.0678 mL
    10 mM 0.0534 mL 0.2670 mL 0.5339 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]. Kopansky E, et al. Peptide-directed HPMA copolymer-doxorubicin conjugates as targeted therapeutics for colorectal cancer. J Drug Target. 2011 Dec;19(10):933-43.

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