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PR5-LL-CM01

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

PR5-LL-CM01 

PR5-LL-CM01 是一种有效的 (PRMT5) 抑制剂 (IC50= 7.5 μM)。PR5-LL-CM01 具有抗肿瘤活性。

PR5-LL-CM01

PR5-LL-CM01 Chemical Structure

CAS No. : 1005307-86-7

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生物活性

PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies[1].

体外研究
(In Vitro)

PR5-LL-CM01 has a range of IC50 at 2-4 μM in PDAC cells (PANC1, MiaPaCa2 and AsPC1, and a range of IC50 at 10-11 μM in CRC cells (HT29, HCT116 and DLD1). PR5-LL-CM01 has higher efficacy to specifically inhibit cancer cells and demonstrated low toxicity in normal cells. PR5-LL-CM01 strongly inhibited colony forming ability in both PANC1 and HT29 cells[1].
PR5-LL-CM01 inhibits NF-κB activation and its target gene expression in PDAC and CRC cells[1].
PR5-LL-CM01 (0-15 μM) dramatically decreases TNFα and IL8 expression in both PANC1 and HT29 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.
体内研究
(In Vivo)

PR5-LL-CM01 (20mg/kg; i.p.; 3 times per week) displays significant anti-tumor effect[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: 6-8 weeks old Male NSG mice (bearing PANC1 or HT29 cells)[1]
Dosage: 20 mg/kg (drug stock dissolved in 1:1 Cremophor:ethanol solution)
Administration: Intraperitoneally 3 times per week; 32 days (PANC1 model); 10 days (HT29 model)
Result: Led to significant tumor inhibition in both PANC1 and HT29 xenografted mice. Did not visibly affect the mice body weight.

分子量

401.51

Formula

C23H27N7
CAS 号

1005307-86-7
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]. Prabhu L, et al. Adapting AlphaLISA high throughput screen to discover a novel small-molecule inhibitor targeting protein arginine methyltransferase 5 in pancreatic and colorectal cancers. Oncotarget. 2017;8(25):39963-39977.

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多肽定制Présure. 10. 145-148 编码

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上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Présure. 10. 145-148
编码
别名 Présure. 10. 145-148
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） AYFYPEL
序列（三字母缩写） Ala-Tyr-Phe-Tyr-Pro-Glu-Leu
基本描述
溶解度
分子量 902.02
化学式 C46H59N7O12
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Présure. 10. 145-148 编码
Figures Présure. 10. 145-148 编码
Reference
C端
N端
化学桥

PR-924

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

PR-924 

PR-924 是一种选择性三肽环氧酮免疫蛋白酶亚单位 LMP-7 的抑制剂，IC50 为 22 nM。PR-924 共价修饰蛋白酶体的 N 端苏氨酸活性位点。PR-924 在多发性骨髓瘤细胞中抑制细胞生长并触发凋亡 (apoptosis)，并具有抗肿瘤活性。

PR-924

PR-924 Chemical Structure

CAS No. : 1416709-79-9

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生物活性

PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities[1][2].

IC50 & Target

IC50: 22 nM (LMP7), 8.2 μM (LMP2)[2]
体外研究
(In Vitro)

PR-924 (1-20 μM; 24-72 hours; MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells) treatment significantly decreases the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 μM for 48 h)[1].
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells[1].
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein, without altering Bax or MCL-1 protein levels[1].
PR-924 induces BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondria-mediated apoptotic signaling pathways via cyto-c release[1].

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

Cell Viability Assay[1]

Cell Line: MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells
Concentration: 1-20 μM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Significantly decreased the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 μM for 48 h).

Apoptosis Analysis[1]

Cell Line: MM.1S and MM.1R cells
Concentration: 3 μM
Incubation Time: 48 hours
Result: Triggered a significant increase in the Annexin V+/PI-apoptotic cell population.

Western Blot Analysis[1]

Cell Line: MM.1S and MM.1R cells
Concentration: 3 μM
Incubation Time: 48 hours
Result: Triggered activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein.

体内研究
(In Vivo)

PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment significantly inhibits tumour growth in human plasmacytoma xenografts[1].
PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival[1].

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

Animal Model: CB-17 SCID-mice injected with MM.1S cells[1]
Dosage: 6 mg/kg
Administration: Intravenous injection; twice a week; for 21 days
Result: Inhibited tumour growth in human plasmacytoma xenografts.

分子量

618.72

Formula

C37H38N4O5
CAS 号

1416709-79-9
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]. Singh AV, et al. PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo. Br J Haematol. 2011 Jan;152(2):155-63.

    [2]. Parlati F, et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. Blood. 2009 Oct 15;114(16):3439-47.

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Carfilzomib(Synonyms: 卡非佐米; PR-171)

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Carfilzomib (Synonyms: 卡非佐米; PR-171)

Carfilzomib (PR-171) 是不可逆的蛋白酶体 (proteasome) 抑制剂，其在ANBL-6和RPMI 8226细胞中的 IC50 为5 nM。

Carfilzomib(Synonyms: 卡非佐米; PR-171)

Carfilzomib Chemical Structure

CAS No. : 868540-17-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥1010 In-stock
10 mg ￥1400 In-stock
50 mg ￥3600 In-stock
100 mg ￥5900 In-stock
200 mg ￥9400 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Carfilzomib 相关产品

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  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus

生物活性

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

IC50 & Target

IC50: 5 nM (Proteasome)
体外研究
(In Vitro)

Carfilzomib displays preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM and above and little or no effect on the PGPH and T-L activities at doses up to 100 nM. Carfilzomib decreases the viability of ANBL-6, RPMI 8226 cells, U266 and KAS-6/1 cells with an IC50 less than 5 nM. Carfilzomib overcome Dex resistance, in that MM1.R cells reveals an IC50 of 15.2 nM, less than the value of 29.3 nM for parental MM1.S cells[1]. Co-treatment with carfilzomib and HDACIs leads to synergistic induction of cell death in various mantle cell lymphoma lines and primary mantle cell lymphoma cells. Combined treatment with carfilzomib or ONX0912 with vorinostat in HF-4B and Granta cells sharply increases caspase activation, PARP cleavage, JNK activation, MnSOD2 induction, and DNA damage[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Carfilzomib (2.0 mg/kg, i.v.) in conbination with 70 mg/kg vorinostat virtually abrogates tumor growth in Granta-luciferace cell xenograft flank model. Combined treatment results in a pronounced reduction in bioluminescence compared to animals treated with single agents or controls with minimal toxicity[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

719.91

Formula

C40H57N5O7
CAS 号

868540-17-4
中文名称

卡非佐米
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

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

DMF : ≥ 100 mg/mL (138.91 mM)

DMSO : 50 mg/mL (69.45 mM; Need ultrasonic)

* “≥” 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 1.3891 mL 6.9453 mL 13.8906 mL
5 mM 0.2778 mL 1.3891 mL 2.7781 mL
10 mM 0.1389 mL 0.6945 mL 1.3891 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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 (3.47 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.47 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 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 (3.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.47 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。

  • 3.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90.

    [2]. Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2011 Sep;10(9):1686-97.
Cell Assay
[1]

WST-1 is used to determine the effects of proteasome inhibitors on cell proliferation according to the manufacturer’s protocol. The inhibition of proliferation is calculated in relation to parallel control cells that receive vehicle alone and tabulated in KaleidaGraph 3.0.1 or Excel 2000. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR=IC50(resistant cells)/IC50(sensitive cells).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Animal studies are performed utilizing Beige-nude-XID mice. 10×106 Granta514 cells are pelleted, washed twice with 1X PBS, injected subcutaneously into the right flank. Once the tumors are visible, 5 to 6 mice are treated with carfilzomib±vorinostat and progress of tumor growth or regression is monitored. Stock vorinostat and carfilzomib is dissolved in DMSO and 10% sulfobutylether betacyclodextrin in 10 mM citrate buffer pH respectively. They are stored in −80°C in small aliquots and diluted before injection.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90.

    [2]. Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2011 Sep;10(9):1686-97.

PR-619

发表于由

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

PR-619  纯度: 98.89%

PR-619 是一种 DUB 抑制剂，作用于 USP4，USP8，USP7，USP2 和 USP5，EC50 分别为 3.93，4.9，6.86，7.2 和 8.61 μM。PR-619 可诱导内质网应激和内质网应激相关的凋亡。

PR-619

PR-619 Chemical Structure

CAS No. : 2645-32-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥880 In-stock
10 mg ￥800 In-stock
50 mg ￥2300 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

PR-619 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Ubiquitination Compound Library
  • Endoplasmic Reticulum Stress Compound Library

生物活性

PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis[1][2][3][4].

IC50 & Target

EC50: 3.93 μM (USP4), 4.9 μM (USP8), 6.86 μM (USP7), 7.2 μM (USP2), 8.61 μM (USP5)[1]
体外研究
(In Vitro)

PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation[2].
PR-619 affects the microtubule network and led to the accumulation of small punctuated tau deposits around. PR-619 causes the dephosphorylation of tau[3].
PR-619 (7-12.5 μM) causes an increase in the abundance of ubiquitinated proteins within 24 h. PR-619 leads to the induction of heat shock proteins and to an increase of ubiquitinated proteins[3].
PR-619 (9 μM) affects the organization of the microtubule network in OLN-t40 cells[3].
PR-619 (5, 7.5, and 10 μM) induces ER Stress and ER-Stress related apoptosis on T24 and BFTC-905 cells. PR-619 induces polyubiquitination, Bcl-2 downregulation, and concurrent PARP cleavage in a dose-dependent manner. PR-619 induces G0/G1 arrest in UC cells[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 Cytotoxicity Assay[1]

Cell Line: OLN-t40 cells.
Concentration: 0-10 μM.
Incubation Time: 24 hours.
Result: Exerted concentration-dependent cytotoxicity in a very narrow concentration range of 7-10 μM.

体内研究
(In Vivo)

PR-619 (10 mg/kg/day) enhances the antitumor effect of Cisplatin on a Cisplatin-Naïve and Cisplatin-resistant UC Xenograft of nude mice[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.

Animal Model: Nude mice[4].
Dosage: 10 mg/kg/day (Cisplatin combined).
Administration: Intraperitoneally.
Result: Enhanced the antitumor effect of Cisplatin.

分子量

223.28

Formula

C7H5N5S2
CAS 号

2645-32-1
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 : ≥ 21 mg/mL (94.05 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 4.4787 mL 22.3934 mL 44.7868 mL
5 mM 0.8957 mL 4.4787 mL 8.9574 mL
10 mM 0.4479 mL 2.2393 mL 4.4787 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 (11.20 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (11.20 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 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

*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]. Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12.

    [2]. Bertuccio CA, et al. Anterograde trafficking of KCa3.1 in polarized epithelia is Rab1- and Rab8-dependent and recycling endosome-independent. PLoS One. 2014 Mar 14;9(3):e92013.

    [3]. Seiberlich V, et al. The small molecule inhibitor PR-619 of deubiquitinating enzymes affects the microtubule network and causes protein aggregate formation in neural cells: implications for neurodegenerative diseases. Biochim Biophys Acta. 2012 Nov;1823(1

    [4]. Kuan-Lin Kuo, et al. The Deubiquitinating Enzyme Inhibitor PR-619 Enhances the Cytotoxicity of Cisplatin via the Suppression of Anti-Apoptotic Bcl-2 Protein: In Vitro and In Vivo Study. Cells. 2019 Oct 17;8(10):1268.

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

PR-104A(Synonyms: SN 27858)

发表于由

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

PR-104A (Synonyms: SN 27858) 纯度: 98.17%

PR-104A (SN 27858) 是磷酸盐前药 PR-104 的醇代谢物。PR-104A 是一种缺氧选择性的 DNA 交联剂/DNA 损伤剂，也是一种细胞毒素。具有抗肿瘤活性。PR-104A 在缺氧条件下通过 1-电子 NADPH:细胞色素 P450 氧化还原酶代谢。可用于复发/难治性 T 系急性淋巴细胞白血病 (T-ALL) 的研究。

PR-104A(Synonyms: SN 27858)

PR-104A Chemical Structure

CAS No. : 680199-06-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4940 In-stock
5 mg ￥4500 In-stock
10 mg ￥8000 In-stock
25 mg ￥16500 In-stock
50 mg ￥25500 In-stock
100 mg ￥38000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

PR-104A 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Drug Metabolite Library

生物活性

PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity[1]. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL)[2].

体外研究
(In Vitro)

PR-104A (1-100 uM) shows antiproliferative potency in a panel of 10 human carcinoma cell lines following 4 hours exposures under aerobic and hypoxic conditions with the lowest IC50 (0.51 μM) in H460 non-small cell lung cancer cells and highest (7.3 μM) in PC3 prostate cells[1].
The phosphate ester PR-104 is rapidly converted in vivo to the alcohol PR-104A, a nitrogen mustard prodrug that is metabolised to hydroxylamine (PR-104H) and amine (PR-104M) DNA crosslinking agents by one-electron reductases in hypoxic cells and by aldo-keto reductase 1C3 independently of oxygen[3].

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: HT29 , HCT116, C33A SiHa A549, H460, H1299 ,PC3,SKOV3, A375 cells
Concentration: 0, 1, 10, 100 uM
Incubation Time: 4 hours under aerobic or hypoxic conditions
Result: The lowest IC50 (0.51 μM) in H460 non-small cell lung cancer cells and highest (7.3 μM) in PC3 prostate cells.

体内研究
(In Vivo)

The phosphate ester “pre-prodrug” PR-104 is well tolerated in mice and converted rapidly to the corresponding prodrug PR-104A. H460 xenografts shows significant sensitivity to PR-104 (total dose 3.2 mmol/kg)[1].

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

Animal Model: Specific pathogen-free homozygous nude (CD1-Foxn1nu) mice with H460 xenografts[1]
Dosage: Daily (0.23 mmol/kg/dose; qd ×14) or weekly (1.07 mmol/kg/dose; qw ×3)
Administration: I.p.
Result: The single-agent activity against H460 tumors refractory to docetaxel, cisplatin, gemcitabine, and cyclophosphamide was particularly striking.
Compared a daily (qd ×14) versus weekly (qw ×3) schedule against the chemoresistant H460 xenograft model using the same total dose (3.2 mmol/kg) over 14 days, which was well tolerated using both schedules.

分子量

499.29

Formula

C14H19BrN4O9S
CAS 号

680199-06-8
运输条件

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

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (500.71 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0028 mL 10.0142 mL 20.0284 mL
5 mM 0.4006 mL 2.0028 mL 4.0057 mL
10 mM 0.2003 mL 1.0014 mL 2.0028 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, stored under nitrogen)。-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: ≥ 6.25 mg/mL (12.52 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (12.52 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 62.5 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: ≥ 6.25 mg/mL (12.52 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (12.52 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 62.5 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: ≥ 6.25 mg/mL (12.52 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (12.52 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 62.5 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Adam V Patterson, et al. Mechanism of action and preclinical antitumor activity of the novel hypoxia-activated DNA cross-linking agent PR-104. Clin Cancer Res. 2007 Jul 1;13(13):3922-32.

    [2]. Donya Moradi Manesh, et al. AKR1C3 is a biomarker of sensitivity to PR-104 in preclinical models of T-cell acute lymphoblastic leukemia. Blood. 2015 Sep 3;126(10):1193-202.

    [3]. McKeage MJ, et al. A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients. BMC Cancer. 2011;11:432. Published 2011 Oct 7.

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

日本ATAGO（爱拓）-PR-301αPALETTE|PR-201αPALETTE数显折射计

发表于由

【简单介绍】

PR-301αPALETTE|PR-201αPALETTE数显折射计 日本ATAGO（爱拓）专业制造，品质保证，能满足您不同环境的实验需求。

【详细说明】

PR-301αPALETTE|PR-201αPALETTE数显折射计

PR-301αPALETTE系列数显折射计

这产品是以PR-301为基础制造的新产品.新增加的功能与PR-101, PR-201同样.测量范围为BRIX 45.0 – 90.0%.它适用于测量豆沙, 果子冻及原料液糖.
*以标准液态规格LG （ RE-9325 ）订定刻度。
型号
PR-301α
货号
3462
测量范围
糖度（Brix） 45.0 至 90.0%
小显示单位
糖度（Brix） 0.1%
测量准确度
糖度（Brix） ±0.1%
（10 至 30°C）
测量温度
10 至 40°C
（自动温度补偿）
环境温度
10 至 40°C
电源
006P 蓄电池 （ 9V ）
保护等级
IP64 无尘且对泼溅的水具防护作用
尺寸重量
17×9×4公分, 300公克
（不含零件的重量）
配件
标准液 LG, 测量用纸
选择性配件
• 标准液 LG （ 7ml ） : RE-9325
• 标准液用测量用纸 : RE-9320
选件
• 50% 蔗糖溶液 （±0.05%） : RE-110050
• 60% 蔗糖溶液 （±0.05%） : RE-110060
PR-201αPALETTE系列数显折射计
这产品是以PR-201为基础制造的新产品.新增加的功能与PR-101α同样.测量范围为BRIX 0.0 – 60.0%.它适用于测量果酱,浓缩果汁及冷却液.
型号
PR-201α
货号
3452
测量范围
糖度（Brix） 0.0 至 60.0%
小显示单位
糖度（Brix） 0.1%
测量准确度
糖度（Brix） ±0.1%
测量温度
10 至 40°C
（自动温度补偿）
环境温度
10 至 40°C
电源
006P 蓄电池 （ 9V ）
保护等级 
IP64 无尘且对泼溅的水具防护作用
尺寸重量
17×9×4公分, 300公克
（不含零件的重量）
选件
• 10% 蔗糖溶液 （±0.03%） : RE-110010
• 20% 蔗糖溶液 （±0.03%） : RE-110020
• 30% 蔗糖溶液 （±0.03%） : RE-110030
• 40% 蔗糖溶液 （±0.04%） : RE-110040
• 50% 蔗糖溶液 （±0.05%） : RE-110050
• 60% 蔗糖溶液 （±0.05%） : RE-110060
 
上海金畔生物科技有限公司：
：
 
：崔
：azlqxb@.cn
：
：kehuai.testmart.cn
 

 

PR-32α PALETTE|PR-101αPALETTE|PR-RI PALETTE数显折射计

发表于由

【简单介绍】

PR-32α PALETTE|PR-101αPALETTE|PR-RI PALETTE数显折射计 性能稳定，品质保证，能满足您不同环境的实验需求。

【详细说明】

PR-32α PALETTE|PR-101αPALETTE|PR-RI PALETTE数显折射计

PR-32αPALETTE系列数显折射计

新型 Paletteα（alpha） 系列实现精度改良为 Brix ±0.1%! Paletteα（alpha） 系列既可测量果汁•食品•饮料等Brix，又可测量化工液体浓度如切削油•清洗液•不冻液等。
Paletteα（alpha） 系列可设置客户刻度，客户自己预设系数 [浓度=Brix x 系数 ]就可直读此样品的浓度。另外，Paletteα（alpha） 系列采用新功能 “External-Light-Interference” （ELI） *，可防止强烈外光下的误测量，可在外边·窗边时的测量也得到稳定测量结果。
型号
PR-32α
货号
3405
测量范围
糖度（Brix） 0.0 至 32.0%
小显示单位
糖度（Brix） 0.1%
测量准确度
糖度（Brix） ±0.1%
测量温度
5 至 40°C
（自动温度补偿）
环境温度
5 至 40°C
电源
006P 蓄电池 （ 9V ）
保护等级
IP64 无尘且对泼溅的水具防护作用
尺寸重量
17×9×4公分, 300公克
（不含零件的重量）
选件
• EXTRACTOR : RE-29401
• 10% 蔗糖溶液 （±0.03%） : RE-110010
• 20% 蔗糖溶液 （±0.03%） : RE-110020
• 30% 蔗糖溶液 （±0.03%） : RE-110030
PR-101αPALETTE系列数显折射计
这产品是以PR-101为基础制造的新产品,在携带式产品里面实现了±0.1%的高精度.它适合测量果汁,食品,饮料及水溶性切削油,清洗液,不冻液等工业用液体,各种药品的浓度.它具有可直接读出用户标度的功能及温度表示功能.还具有ELI功能. 有了ELI功能, 如该仪器受较强光线,显示出NNN.有了这个显示, 用手盖住菱镜再按开始键就可以了. （ELI功能正在申请中）
Model
PR-101α（ alpha ）
型号
3442
测量范围
糖度（Brix） 0.0 至 45.0%
小显示单位
糖度（Brix） 0.1%
测量准确度
糖度（Brix） ±0.1%
测量温度
5 至 40°C（自动温度补偿）
环境温度
5 至 40°C
电源
006P 蓄电池 （ 9V ）
保护等级
IP64 无尘且对泼溅的水具防护作用
尺寸重量
17×9×4公分, 300公克
（不含零件的重量）
选件
• EXTRACTOR : RE-29401
• 10% 蔗糖溶液 （±0.03%） : RE-110010
• 20% 蔗糖溶液 （±0.03%） : RE-110020
• 30% 蔗糖溶液 （±0.03%） : RE-110030
• 40% 蔗糖溶液 （±0.04%） : RE-110040
PR-RI PALETTE系列数显折射计
我们ATAGO产品袖珍型产品中商品的PAL系列增加了新产品, 就是测量折射率的PAL-RI.适合在药品及化工制品等以折射率来管理产品质量的过程中使用.
型号
PR-RI
货号
3480
测量范围
折射指数（nD）
1.3306 至 1.4436
溶解值
折射指数（nD） 0.0001
测量准确度
折射指数（nD）±0.0002
（在20度摄氏使用水时）
环境温度
10 至 40°C
测量温度
5 至 45°C
（溶解值 1°C ）
样本量
0.3 毫升
测量时间
3 秒
电源
006P 蓄电池 （ 9V ）
保护等级 
IP64 无尘且对泼溅的水具防护作用。
尺寸重量
17×9×4公分, 300公克
（不含零件的重量）
上海金畔生物科技有限公司：
：
 
：崔
：azlqxb@.cn
：
：kehuai.testmart.cn