月度归档：2023年10月

Boc-C5-O-C5-O-C6-Cl(Synonyms: PROTAC Linker 2)

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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。

Boc-C5-O-C5-O-C6-Cl (Synonyms: PROTAC Linker 2) 纯度: ≥95.0%

Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) 是用于将酪氨酸激酶 (TKI) 抑制剂连接到E3招募配体上的一种 PROTAC 连接体。

Boc-C5-O-C5-O-C6-Cl(Synonyms: PROTAC Linker 2)

Boc-C5-O-C5-O-C6-Cl Chemical Structure

CAS No. : 1835705-52-6

规格 价格 是否有货 数量
100 mg ￥4500 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.

IC50 & Target

Alkyl/ether

 

分子量

393.00

Formula

C21H41ClO4
CAS 号

1835705-52-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Lai AC, et al. Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL. Angew Chem Int Ed Engl. 2016 Jan 11;55(2):807-10.

    [2]. ARYL SULFONOHYDRAZIDES. US 20170121321 A1.

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钩吻碱对照品

发表于由
钩吻碱对照品

  【编号】：PR0629

  【产品名称】：钩吻碱对照品

  【规格】：10mg

  【用途】：

　　钩吻碱对照品

　　编号：PR0629
　　英文名称：Gelsemine
　　中文别名: 钩吻素甲
　　Cas 号: 509-15-9
　　分 子 式：C20H22N2O2
　　分 子 量：322.408
　　植物来源：断肠草
　　来源: Alkaloid from Gelsemium sempervirens, Gelsemium elegans and Mostuea stimulans (Loganiaceae)
　　纯度: 95%~99%
　　分析方法: HPLC-DAD or/and HPLC-ELSD
　　鉴定方法: 质谱（Mass）, 核磁（NMR）
　　包装: 棕色小玻璃瓶，标准包装10mg，20mg，50mg；可以按客户需求包装。
　　类别：上海金畔生物科技有限公司，天然提取物
　　作为标准品，对照品或者供研究用，不能直接用于人体。

Aprotinin(Synonyms: 抑肽酶)

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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。

Aprotinin (Synonyms: 抑肽酶) 纯度: ≥98.0%

Aprotinin是分离自牛肺的丝氨酸蛋白酶 (BPTI) 抑制剂，对胰蛋白酶和胰凝乳蛋白酶胰凝乳蛋白酶的 Ki 值分别为0.06 pM和9 nM。

Aprotinin(Synonyms: 抑肽酶)

Aprotinin Chemical Structure

CAS No. : 9087-70-1

规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥2865 In-stock
10 mg ￥500 In-stock
50 mg ￥2000 In-stock
100 mg ￥3200 In-stock
200 mg   询价  
500 mg   询价  

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  • Rare Diseases Drug Library

生物活性

Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.

IC50 & Target

Ki: 0.06 pM (Trypsin), 9 nM (Chymotrypsin)[1]
体外研究
(In Vitro)

Aprotinin, a serine protease inhibitor isolated from bovine lung, is a complex protease inhibitor that is an antifibrinolytic, inhibits contact activation, and decreases the inflammatory response to cardiopulmonary bypass[2]. Aprotinin inhibits trypsin (bovine, Ki= 0.06 pM), chymotrypsin (bovine, Ki= 9 nM), plasmin (human, 0.23 nM)[1]. Aprotinin is also a competitive protein inhibitor of NOS activity. It inhibits NOS-I and NOS-II with Ki values of 50 μM and 78 μM, respectively[3]. Aprotinin significantly inhibits fibrinolysis with an IC50 of 0.16±0.05 μM[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.
体内研究
(In Vivo)

High dose aprotinin can reduce blood loss and transfusion requirements associated with primary cardiac procedures such as coronary artery bypass graft (CABG) or heart valve replacement surgery[5]. Aprotinin inhibits thrombus formation in a dose-dependent manner. Aprotinin at a dose of 1.5 mg kg-1 (bolus) and 3 mg kg-1 h-1 infusion (maintenance infusion) causes a tendency towards a reduction in bleeding time. Aprotinin significantly reduces the bleeding time starting at a dose of 3 mg kg-1 bolus plus 6 mg kg-1 h-1 showing a reduction of approximately 84%±2.9%. At the highest dose of 5 mg kg-1 and 10 mg kg-1 h-1, the strongest effects are observed[4]. Aprotinin may affect tumor necrosis factor-alpha (TNF) levels. Soluble TNFRI levels are significantly increased following I/R in the aprotinin treated wild type mice and not detected in all TNFRInull mice[6].

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

分子量

6511.44

Formula

C284H432N84O79S7
CAS 号

9087-70-1
Sequence

Arg-Pro-Asp-Phe-Cys-Leu-Glu-Pro-Pro-Tyr-Thr-Gly-Pro-Cys-Lys-Ala-Arg-Ile-Ile-Arg-Tyr-Phe-Tyr-Asn-Ala-Lys-Ala-Gly-Leu-Cys-Gln-Thr-Phe-Val-Tyr-Gly-Gly-Cys-Arg-Ala-Lys-Arg-Asn-Asn-Phe-Lys-Ser-Ala-Glu-Asp-Cys-Met-Arg-Thr-Cys-Gly-Gly-Ala(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51)
Sequence Shortening

RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51)
中文名称

抑肽酶；抑胰肽酶；屈来密多
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 : 100 mg/mL (15.36 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.1536 mL 0.7679 mL 1.5358 mL
5 mM 0.0307 mL 0.1536 mL 0.3072 mL
10 mM 0.0154 mL 0.0768 mL 0.1536 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]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.

    [2]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

    [3]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5

    [4]. Sperzel M, et al. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31.

    [5]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83.

    [6]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62.
Animal Administration
[4][6]

Rats: Male Wistar rats (180-220 g) are used in the study. Aprotinin is dissolved in physiological saline. Aprotinin is administered by bolus injection followed by a maintenance infusion. The doses given are 1.5 mg kg-1 and 3 mg kg-1 h-1, 3mg kg-1 and 6 mg kg-1 h-1 up to 5 mg kg-1 and 10 mg kg-1 h-1. Plasma concentrations for the two agents are assessed by pharmacokinetic studies in rats[4].

Mice: An intact mouse model of ischemia/reperfusion (30 min-I/60 min-R) is used and left ventricular peak + dP/dt is measured in wild type mice (WT, C57BL/6; n=10), WT mice with aprotinin (4mL/kg; n=10), transgenic mice devoid of the TNFRI (TNFRInull; n=10), and TNFRInull with aprotinin (n=10)[6].

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]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.

    [2]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

    [3]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5

    [4]. Sperzel M, et al. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31.

    [5]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83.

    [6]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62.

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Canagliflozin hemihydrate(Synonyms: JNJ 28431754 hemihydrate)

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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。

Canagliflozin hemihydrate (Synonyms: JNJ 28431754 hemihydrate) 纯度: 99.95%

Canagliflozin hemihydrate (JNJ28431754 hemihydrate) 是一种选择性的 SGLT2 抑制剂，作用于表达 mSGLT2，rSGLT2 和 hSGLT2 的 CHO细胞，IC50 分别为 2 nM，3.7 nM 和 4.4 nM。

Canagliflozin hemihydrate(Synonyms: JNJ 28431754 hemihydrate)

Canagliflozin hemihydrate Chemical Structure

CAS No. : 928672-86-0

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 ￥1045 In-stock
5 mg ￥950 In-stock
10 mg ￥1400 In-stock
50 mg ￥2900 In-stock
100 mg ￥4200 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[1].

IC50 & Target

IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells)[1]
体外研究
(In Vitro)

Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice[1].
Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF 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: Diet-induced obese, insulin resistantmice (DIO) Mice[1]
Dosage: 30 mg/kg
Administration: Oral gavage; daily; 4 weeks
Result: Reduced BG levels, respiratory exchange ratio, and body weight gain.
Animal Model: Male Zucker fatty (ZF) obese, insulin resistant rats[1]
Dosage: 3 mg/kg
Administration: Oral gavage; daily; 3 weeks
Result: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.

Clinical Trial

分子量

453.52

Formula

C24H26FO5.5S
CAS 号

928672-86-0
中文名称

卡格列净半水合物；坎格列净半水合物
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 (220.50 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 2.2050 mL 11.0249 mL 22.0497 mL
5 mM 0.4410 mL 2.2050 mL 4.4099 mL
10 mM 0.2205 mL 1.1025 mL 2.2050 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 (5.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.51 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 (5.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.51 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 (5.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.51 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]. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555.

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Pomalidomide(Synonyms: 泊马度胺; CC-4047)

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。

Pomalidomide (Synonyms: 泊马度胺; CC-4047) 纯度: 99.85%

Pomalidomide 是第三代免疫调节剂，以分子胶的方式作用。Pomalidomide 与 E3 连接酶 cereblon 相互作用，诱导必需的 Ikaros 转录因子的降解。

Pomalidomide(Synonyms: 泊马度胺; CC-4047)

Pomalidomide Chemical Structure

CAS No. : 19171-19-8

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 ￥616 In-stock
10 mg ￥560 In-stock
50 mg ￥840 In-stock
100 mg ￥1080 In-stock
200 mg ￥1200 In-stock
500 mg ￥1400 In-stock
1 g ￥1800 In-stock
5 g ￥4500 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

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生物活性

Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

IC50 & Target[5]

Cereblon

 

体外研究
(In Vitro)

Pomalidomide also inhibits Whole Blood TNF-α with IC50 of 25 nM[1]. Exposure of lymphoma cells to Pomalidomide (CC-4047) leads to 40% decrease in cell proliferation when compared with vehicle-treated controls. Pomalidomide inhibits by 40% the DNA synthesis of Raji cells (P=0.036)[2]. In both CD4+ and CD8+ cells, Pomalidomide (CC-4047) is the most potent IL-2-elevator, followed by CC-6032 and CC-5013. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10, and slightly more potent than CC-5013 at elevating IFN-γ[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)

The administration of Pomalidomide (CC-4047) for two consecutive days before mAb therapy enhances the antitumor activity of Rituximab and doubled the median survival of lymphoma-bearing mice. Statistically, significant differences are observed between animals treated with Rituximab versus Pomalidomide+Rituximab. The median survival time of animals treated with Pomalidomide and Rituximab is longer (median survival, 74 days; 95% CI, 70-78) than those treated with Rituximab monotherapy (median survival, 38 days; 95% CI, 26-50; log-rank test, P=0.002). The administration of CC-5013 or Pomalidomide for two consecutive days leads to a significant increase in the number of circulating NK cells as shown by flow cytometry analysis, in lymphoma-bearing SCID mice[2]. Following a 50 mg/kg PO administration of Pomalidomide (POM) to rats, unbound concentrations in blood reach a Cmax value of 1100±82 ng/mL at 4.6±2.4 hours, with a concomitant AUC(0-10) value of 6800±2000 ng•hr/mL. Unbound POM in the brain, however, has a Cmax value of 430±63 ng/mL at 4.1±1.5 hours and an AUC(0-10) value of 2700±740 ng•hr/mL, giving an unbound AUCbrain to AUCblood ratio of 0.39±0.03. These values are consistent with excellent blood-brain-barrier penetration. The results obtained in this study are consistent with those seen in a concurrent study looking at whole brain POM content following its oral administration to 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.
Clinical Trial

分子量

273.24

Formula

C13H11N3O4
CAS 号

19171-19-8
中文名称

泊马度胺
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 : 83.33 mg/mL (304.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6598 mL 18.2989 mL 36.5979 mL
5 mM 0.7320 mL 3.6598 mL 7.3196 mL
10 mM 0.3660 mL 1.8299 mL 3.6598 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： 0.5% CMC-Na  0.5% Tween-80

    Solubility: 10 mg/mL (36.60 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.15 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.15 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]. Zhu YX, et al. Molecular mechanism of action of the immune-modulatory drugs, thalidomide, lenalidomide and pomalidomide in multiple myeloma. Leuk Lymphoma. 2013 Apr;54(4):683-7.

    [2]. Hernandez-Ilizaliturri FJ1, et al. Immunomodulatory drug CC-5013 or CC-4047 and rituximab enhance antitumor activity in a severe combined immunodeficient mouse lymphoma model. Clin Cancer Res. 2005 Aug 15;11(16):5984-92.

    [3]. Schafer PH, et al. Enhancement of cytokine production and AP-1 transcriptional activity in T cells by thalidomide-related immunomodulatory drugs. J Pharmacol Exp Ther. 2003 Jun;305(3):1222-32.

    [4]. Li Z, et al. Pomalidomide shows significant therapeutic activity against CNS lymphoma with a major impact on the tumor microenvironment in murine models. PLoS One. 2013 Aug 5;8(8):e71754.

    [5]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

    [6]. Liu D, et al. Tumour necrosis factor-α inhibits hepatic lipid deposition through GSK-3β/β-catenin signaling in juvenile turbot (Scophthalmus maximus L.). Gen Comp Endocrinol. 2016 Mar 1;228:1-8.
Cell Assay
[2]

Lymphoma cell lines are placed in 96-well plates (1×105 cells per well) and exposed to escalating concentrations of CC-5013, Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL), or vehicle control single agents or in combination with Rituximab or Trastuzumab (isotype), at a final antibody concentration of 10 μg/mL. The final concentration is adjusted to 200 μL with 10% RPMI. The cell lines are incubated at 37°C and 5% CO2 for 24 and 48 hours. Following 24 or 48 hours, 1 μCi per well of [3H]-thymidine is added and cells are incubated for 18 hours more. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter. Each experiment is done in triplicate at three different times; results are presented as the mean of counts per minute (cpm) at 24 and 48 hours±SD[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 Administration
[2][4]

Mice[2]
Six- to 8-week-old SCID mice are used for this purpose. On day 0, all the animals receive 1×106 Raji cells via tail vein injection. After 72 hours of tumor engraftment, the animals are divided into seven cohorts. The first cohort (group A) serve as control and receive no treatment. Groups B and C consist of animals treated with either CC-5013 (0.5 mg/kg) or Pomalidomide (0.5 mg/kg) given i.p. on days +3, +4, +8, +9, +13, +14, +18, and +19. Groups D and E are treated with Rituximab or Trastuzumab (isotype control) monotherapy given via tail vein injection at 10 mg/kg on days +5, +10, +15, and +20. Finally, groups F and G consist of animals treated with Rituximab in combination with CC-5013 (group E) or Pomalidomide (group G). IMiDs are given i.p. for two consecutive days before each dose of Rituximab. After completion of therapy, animals are observed for a period of 90 days. The end point of the study is survival defined as the time for the development of limb paralysis. Animals that reach the end point or survived after 3 months of observation are sacrificed by cervical dislocation. Pathologic examination of all organs (liver, lung, and brain) is done to detect any residual disease. The experiments are repeated in three separate occasions.
Rats[4]
A total of 3 male CD-IGS rats are used. Pomalidomide is administered as a single PO administration via the stomach cannula, at 50 mg/kg (5 mL/kg) in a 0.5% carboxymethylcellulose/0.25% Tween 80 suspension formulation. Microdialysate is collected in a cooling fraction collector, set at 4°C at intervals of 25 minutes for 10 hours after dosing. To calculate AUC, the corrected concentration of each sample is multiplied by the interval over which the sample is collected; in this case 25 minutes, and divided by 60 minutes per hour. The sum of these values represented the total AUC value over the specified time range. To generate graphs, the concentration at each time point is plotted at the mid-point of each collection interval. Microdialysates are collected at the specified time points and analyzed for Pomalidomide concentration using a LC-MS/MS assay, within 12 hours.

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]. Zhu YX, et al. Molecular mechanism of action of the immune-modulatory drugs, thalidomide, lenalidomide and pomalidomide in multiple myeloma. Leuk Lymphoma. 2013 Apr;54(4):683-7.

    [2]. Hernandez-Ilizaliturri FJ1, et al. Immunomodulatory drug CC-5013 or CC-4047 and rituximab enhance antitumor activity in a severe combined immunodeficient mouse lymphoma model. Clin Cancer Res. 2005 Aug 15;11(16):5984-92.

    [3]. Schafer PH, et al. Enhancement of cytokine production and AP-1 transcriptional activity in T cells by thalidomide-related immunomodulatory drugs. J Pharmacol Exp Ther. 2003 Jun;305(3):1222-32.

    [4]. Li Z, et al. Pomalidomide shows significant therapeutic activity against CNS lymphoma with a major impact on the tumor microenvironment in murine models. PLoS One. 2013 Aug 5;8(8):e71754.

    [5]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

    [6]. Liu D, et al. Tumour necrosis factor-α inhibits hepatic lipid deposition through GSK-3β/β-catenin signaling in juvenile turbot (Scophthalmus maximus L.). Gen Comp Endocrinol. 2016 Mar 1;228:1-8.

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

Vincristine-d3-ester sulfate(Synonyms: Leurocristine-d3-ester sulfate; NSC-67574-d3-ester sulfate; 22-Oxovincaleukoblastine-d3-ester sulfate)

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。

Vincristine-d3-ester sulfate (Synonyms: Leurocristine-d3-ester sulfate; NSC-67574-d3-ester sulfate; 22-Oxovincaleukoblastine-d3-ester sulfate)

Vincristine-d3-ester (Leurocristine-d3-ester) sulfate 是 Vincristine sulfate 的氘代物。Vincristine sulfate是一种抗肿瘤长春花生物碱，抑制有丝分裂纺锤体中的 microtubule 形成，导致中期阶段的分裂细胞停滞。 它与 microtubule 结合的 Ki 为85 nM。

Vincristine-d3-ester sulfate(Synonyms: Leurocristine-d3-ester sulfate; NSC-67574-d3-ester sulfate; 22-Oxovincaleukoblastine-d3-ester sulfate)

Vincristine-d3-ester sulfate Chemical Structure

CAS No. : 1217854-24-4

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Vincristine-d3-ester (Leurocristine-d3-ester) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1] .

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

926.05

Formula

C46H55D3N4O14S
CAS 号

1217854-24-4
中文名称

硫酸长春新碱 ester (硫酸盐)
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]. Jordan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res, 1985. 45(6): p. 2741-7.

    [3]. Gidding, C.E., et al, Vincristine revisited. Crit Rev Oncol Hematol, 1999. 29(3): p. 267-87.

    [4]. Donoso, J.A., et al, Action of the vinca alkaloids vincristine, vinblastine, and desacetyl vinblastine amide on axonal fibrillar organelles in vitro. Cancer Res, 1977. 37(5): p. 1401-7.

    [5]. Horton, J.K., et al. Relationships between tumor responsiveness, vincristine pharmacokinetics and arrest of mitosis in human tumor xenografts. Biochem Pharmacol, 1988. 37(20): p. 3995-4000.

    [6]. Baguley, B.C., et al, Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer, 1991. 27(4): p. 482-7.

    [7]. Zhang D, et al. Co-delivery nanoparticles with characteristics of intracellular precision release drugs for overcoming multidrug resistance. Int J Nanomedicine. 2017 Mar 16;12:2081-2108.

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

德国KGW法兰口杜瓦瓶NF7C/NF8C/NF14C/NF19C/NF11C/NF-S22C

发表于由

【简单介绍】

德国KGW法兰口杜瓦瓶NF7C/NF8C/NF14C/NF19C/NF11C/NF-S22C,法兰连接；密闭、不漏气；NF型为schott法兰口，F型为平法兰口。适合储存液氮、干冰等低温品，也可以在实验室冷冻储存小量样品，有配套的盖子防止蒸发.

【详细说明】

德国KGW法兰口杜瓦瓶NF7C/NF8C/NF14C/NF19C/NF11C/NF-S22C

主要特点：

密闭、不漏气；

耐受过压0.1bar，铝制外壳。满足实验室不同需求；

法兰连接；

3.3硼硅玻璃材质；

适合储存液氮、干冰等低温品，也可以在实验室冷冻储存小量样品，有配套的盖子防止蒸发；

NF型为schott法兰口，F型为平法兰口。


德国KGW法兰口杜瓦瓶NF7C/NF8C/NF14C/NF19C/NF11C/NF-S22C

订货信息：

型号

内容(mL)

内直径/

内高度(mm)

总高度(  （mm)

重量（kg）

Schott法兰口

NF7C

1200

67/400

445

1.0

NW60

NF8C

1700

67/550

610

1.3

NW60

NF11C

2100

77/550

600

2.0

NW60

NF14C

3300

90/660

720

2.9

NW100

NF17C

4100

100/660

720

3.3

NW100

NF19C

5100

110/660

720

3.6

NW100

NF-S22C

8100

138/660

735

5.3

NW150

F0C

200

40/160

215

0.3


F1C

300

47/180

240

0.3


F3C

500

57/200

260

0.5


F6C

800

67/230

295

0.6


F7C

1200

67/340

395

0.8


F9C

1000

77/225

290

0.7


F10C

1500

77/335

395

1.1


F12C

1500

90/235

300

1.1


F13C

2000

90/330

390

1.4


F15C

1500

100/230

300

1.2


F16C

2000

100/280

345

1.4


F18C

2500

110/280

345

1.7


F19C

5000

110/590

660

3.2


F-S21C

4000

138/300

375

2.4


F-S22C

8000

138/590

660

4.6



郑州长城科工贸超低温循环冷却器LT-100-110

发表于由

郑州长城科工贸超低温循环冷却器LT-100-110

  • 品牌 长城科工贸|Greatwall
  • 型号 LT-100-110
  • 商品详情

    主要用于为需冷设备提供超低温循环冷却液体，维持在低温条件下工作的低温反应;可与20L、50L、100L等反应釜配套使用，将反应釜内物料冷却到-70℃、-80℃、-100℃。

    ● 采用微机控制，全数字化中文显示，操作方便。温度显示采用高亮度LED。高低压保护、过载保护、过电流保护功能。

    ● 环保无氟制冷剂，符合欧盟及国家标准。

    ● 制冷系统压缩机、油分离器、电磁阀、膨胀阀等均采用进口品牌。

    ● 蒸发器为全钎焊板式换热器。

    ● 耐低温专用循环泵，低温工况下无泄漏、无堵转现象。

    ● 循环系统采用密闭式循环系统。无挥发保护实验人员健康。

    ● 储液槽及载冷介质全部采用304不锈钢材质，耐腐蚀性好。

    ● 整机稳定可靠，能满足24h以上连续生产对工艺冷源的需求。

    ● 主机冷却方式为风冷。

    ● 外壳为静电喷塑SPCC，防腐效果好。

    型号

    LT-20-80

    LT-50-80

    LT-100-80

    LT-100-110

       使用温度范围（℃）

    -80~-40

    -80~-40

    -80~-40

    -100~-60

       温度稳定性（℃）

    ±2

    ±2

    ±2

    ±2

       最佳环境温度（℃）

    5~25

    5~25

    5~25

    5~25

       电源（V/Hz）

    3~，380V，50Hz

    3~，380V，50Hz

    3~，380V，50Hz

    3~，380V，50Hz

       整机功率（kW）

    4.9

    9.8

    19.3

    38

       制冷剂

    R404A/R23

    R404A/R23

    R404A/R23

    R404A/R23/R14

    制冷量（W）

    -40℃

    2000

    5000

    10000

    –

    -60℃

    1400

    3000

    6000

    –

    -80℃

    450

    1000

    2500

    5500

    -90℃

    –

    –

    –

    3700

    -100℃

    –

    –

    –

    2500

    循环泵

    功率（W）

    280

    280

    280

    2800

    额定流量（L/min）

    30

    30

    30

    50

    压力（bar）

    1.0

    1.0

    1.0

    3.0

    储液槽容积（L）

    10

    10

    24

    100

    外形尺寸（mm）

    1060D×645W×1320H

    1200L×710W×1280H

    1435D×850W×1598H

    2950L×1500W×2385H

       重量（kg）

    235

    350

    600

    1500

    • 灵芝酮三醇对照品

    发表于由
    灵芝酮三醇对照品

      【编号】：PR0621

      【产品名称】：灵芝酮三醇对照品

      【规格】：10mg

      【用途】：

    　　灵芝酮三醇对照品

    　　编号：PR0621
    　　英文名称：Ganodermatriol
    　　CAS No.：105300-28-5
    　　分 子 式：C30H48O3
    　　分 子 量：456.711
    　　类别：上海金畔生物科技有限公司，天然提取物
    　　作为标准品，对照品或者供研究用，不能直接用于人体。

    DMOG(Synonyms: Dimethyloxallyl Glycine)

    发表于由

    DMOG (Synonyms: Dimethyloxallyl Glycine) 纯度: 98.70%

    DMOG (Dimethyloxallyl Glycine) 是具有细胞渗透和竞争性 HIF-PH 抑制剂，可导致蛋白 HIF-1α 的积聚和稳定。DMOG 是 α-ketoglutarate 的类似物并且可以抑制 α-KG 依耐性羟化酶。DMOG 是一种促血管生成剂，在结肠炎和腹泻动物模型中起保护作用。DMOG 可以诱导细胞自噬 (autophagy).

    DMOG(Synonyms: Dimethyloxallyl Glycine)

    DMOG Chemical Structure

    CAS No. : 89464-63-1

    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 ￥715 In-stock
    50 mg ￥650 In-stock
    100 mg ￥990 In-stock
    200 mg ￥1750 In-stock
    500 mg ￥3950 In-stock
    1 g   询价  
    5 g   询价  

    * Please select Quantity before adding items.

    DMOG 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus
    • Epigenetics Compound Library
    • Immunology/Inflammation Compound Library
    • Metabolism/Protease Compound Library
    • Anti-Cancer Compound Library
    • Autophagy Compound Library
    • Reprogramming Compound Library
    • Oxygen Sensing Compound Library
    • Glutamine Metabolism Compound Library
    • Anti-Breast Cancer Compound Library
    • Anti-Cancer Metabolism Compound Library
    • Angiogenesis Related Compound Library
    • Transcription Factor Targeted Library

    生物活性

    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo[1]. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal[2][4]. DMOG induces cell autophagy[5].

    IC50 & Target

    HIF-1α prolyl hydroxylase[1]
    体外研究
    (In Vitro)

    DMOG efficiently suppresses hydroxyproline synthesis in intact cells, but shows only weakly active in the microsomal system[1]. DMOG reduces FGF-2-induced proliferation and cyclin A expression by inhibiting prolyl hydroxylase activity in HPASMC[3].

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

    DMOG inhibits endogenous HIF inactivation, and induces angiogenesis in ischaemic skeletal muscles of mice[2]. Up-regulation of hypoxia-inducible factor-1α by DMOG enhances the cardioprotective effects of ischemic postconditioning in hyperlipidemic rats[4].

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

    175.14

    Formula

    C6H9NO5
    CAS 号

    89464-63-1
    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 : ≥ 50 mg/mL (285.49 mM)

    H2O : 50 mg/mL (285.49 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 5.7097 mL 28.5486 mL 57.0972 mL
    5 mM 1.1419 mL 5.7097 mL 11.4194 mL
    10 mM 0.5710 mL 2.8549 mL 5.7097 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： PBS

      Solubility: 150 mg/mL (856.46 mM); Clear solution; Need ultrasonic

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    • [1]. Baader E, et al. Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues. Biochem J. 1994 Jun 1;300 (Pt 2):525-30.

      [2]. Milkiewicz M, et al. Inhibition of endogenous HIF inactivation induces angiogenesis in ischaemic skeletal muscles of mice. J Physiol. 2004 Oct 1;560(Pt 1):21-6.

      [3]. Schultz K, et al. Prolyl hydroxylase 2 deficiency limits proliferation of vascular smooth muscle cells by hypoxia-inducible factor-1{alpha}-dependent mechanisms. Am J Physiol Lung Cell Mol Physiol. 2009 Jun;296(6):L921-7.

      [4]. Li X, et al. Up-regulation of hypoxia-inducible factor-1α enhanced the cardioprotective effects of ischemic postconditioning in hyperlipidemic rats. Acta Biochim Biophys Sin (Shanghai). 2014 Feb;46(2):112-8.

      [5]. Singh A, et al. Hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitors induce autophagy and have a protective effect in an in-vitro ischaemia model.Sci Rep. 2020 Jan 31;10(1):1597.
    Cell Assay
    [3]

    To analyze DNA synthesis as an index of cellular proliferation, VSMC are plated in 48-well plates (5,000 per square centimeter) in growth medium, incubated overnight, and serum-deprived (1% FCS) for 24 h. Replicate wells are then stored at −70°C for baseline (day 0) cell counts, and fresh medium with or without growth factors is added to the remaining wells, which are incubated 72-96 h in 20 or 5% O2. Days 0 and 3 or 4 cell counts are determined by lysing cells in a buffer containing a fluorescent dye, which has minimal fluorescence by itself but fluoresces when bound to DNA or RNA. Absolute cell numbers are calculated by comparing the fluorescence of specimens with that of a standard curve similarly prepared using a known number of cells.

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

    Two groups of mice (C57Bl6) are used. One group (n=11) receives dimethyloxalylglycine (DMOG) i.p. (8 mg in 0.5 mL saline) on days 1, 3, 5, 7 and 9 while the animals in the other group are injected with sterile saline (0.5 mL) at the same intervals (n=6). A third group is treated with DMOG without ligation (n=4) and four unoperated mice serve as controls. After 11 days mice are terminally anaesthetized and the extensor digitorum longus (EDL) and tibialis anterior (TA) muscles excised.

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

    • [1]. Baader E, et al. Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues. Biochem J. 1994 Jun 1;300 (Pt 2):525-30.

      [2]. Milkiewicz M, et al. Inhibition of endogenous HIF inactivation induces angiogenesis in ischaemic skeletal muscles of mice. J Physiol. 2004 Oct 1;560(Pt 1):21-6.

      [3]. Schultz K, et al. Prolyl hydroxylase 2 deficiency limits proliferation of vascular smooth muscle cells by hypoxia-inducible factor-1{alpha}-dependent mechanisms. Am J Physiol Lung Cell Mol Physiol. 2009 Jun;296(6):L921-7.

      [4]. Li X, et al. Up-regulation of hypoxia-inducible factor-1α enhanced the cardioprotective effects of ischemic postconditioning in hyperlipidemic rats. Acta Biochim Biophys Sin (Shanghai). 2014 Feb;46(2):112-8.

      [5]. Singh A, et al. Hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitors induce autophagy and have a protective effect in an in-vitro ischaemia model.Sci Rep. 2020 Jan 31;10(1):1597.

    EAI045

    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。

    EAI045  纯度: 98.90%

    EAI045是突变体 EGFR 的第四代变构抑制剂，在10 μM ATP时抑制EGFR，EGFRL858R，EGFRT790M 和 EGFRL858R/T790M 的IC50 值分别为1.9，0.019，0.19 和 0.002 μM。

    EAI045

    EAI045 Chemical Structure

    CAS No. : 1942114-09-1

    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 ￥1650 In-stock
    50 mg ￥1500 In-stock
    100 mg ￥2500 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    EAI045 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
    • Anti-Cancer Compound Library
    • Differentiation Inducing Compound Library
    • Anti-Hepatitis C Virus Compound Library
    • Anti-Lung Cancer Compound Library
    • Anti-Pancreatic Cancer Compound Library
    • Angiogenesis Related Compound Library
    • Targeted Diversity Library
    • Anti-Liver Cancer Compound Library
    • Anti-Colorectal Cancer Compound Library

    生物活性

    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.

    IC50 & Target

    EGFR

    1.9 μM (IC50)

    EGFRL858R

    0.019 μM (IC50)

    EGFRT790M

    0.19 μM (IC50)

    EGFRL858R/T790M

    0.002 μM (IC50)

    体外研究
    (In Vitro)

    EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM), but not in HaCaT cells. EAI045 is an inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wild type EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 protein kinases reveals exquisite selectivity; no other kinases are inhibited by more than 20% at 1 μM EAI045[1]. EAI045 has high potency and selectivity for L858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045 decreases but does not completely abolish the EGFR autophosphorylation. In stably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045 shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderate activity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR, EAI045 does not show any activity of inhibiting EGFR phosphorylation. It confirms the selectivity of EAI045 for mutant EGFR[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)

    In a genetically engineered mouse model of L858R/T790Mmutant-driven lung cancer , remarkable tumor regression is observed in L858R/T790M-mutant mice treated with the combination of EAI045 and cetuximab. No response is seen in those mice treated with EAI045 alone. The same effect is seen in both L858R/T790M/C797S- engineered Ba/F3 cells and in mice carrying the L858R/T790M/C797S tumor xenografts. These assays clearly show that EAI045 can overcome resistance from acquired T790M and C797S mutations[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

    383.40

    Formula

    C19H14FN3O3S
    CAS 号

    1942114-09-1
    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 : 100 mg/mL (260.82 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6082 mL 13.0412 mL 26.0824 mL
    5 mM 0.5216 mL 2.6082 mL 5.2165 mL
    10 mM 0.2608 mL 1.3041 mL 2.6082 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 (6.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.52 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 (6.52 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (6.52 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 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 (6.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (6.52 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 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]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32.

      [2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.
    Cell Assay
    [1]

    For the experiment studying the effect of EGF pre-treatment on EAI045 target modulation, H1975 cells are harvested and plated in 0.5% FBS/RPMI Pen/Strep. On the following day, cells are pre-treated with 0.5% FBS/RPMI media with or without 10 ng EGF/mL for 5 minutes. Compound is added and assay is carried out[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: Cetuximab is administrated at 1 mg/mouse every other day by intraperitoneal injection. The TL, TD and TLCS mice are monitored by MRI to quantify lung tumor burden before being assigned to various study treatment cohorts, which are non-blinded and not formally randomized. All treated mice had an equal initial tumor burden. MRI evaluation is repeated every 2 weeks during treatment. The animals are imaged with a rapid acquisition with relaxation enhancement sequence in the coronal and axial planes with a 1-mm slice thickness gating with respiratory rates. The tumor burden volumes are quantified[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]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32.

      [2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.

    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

    Romidepsin(Synonyms: 罗米地辛; FK 228; FR 901228; NSC 630176)

    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。

    Romidepsin (Synonyms: 罗米地辛; FK 228; FR 901228; NSC 630176) 纯度: 99.92%

    Romidepsin (FK 228) 是具有抗肿瘤活性的组蛋白去乙酰化酶 (HDAC) 抑制剂，抑制 HDAC1，HDAC2，HDAC4 和 HDAC6，IC50 值分别为 36 nM，47 nM，510 nM 和 1.4 μM。Romidepsin (FK 228) 由紫色杆菌产生，诱导 G2/M 细胞周期阻滞和凋亡 (apoptosis)。

    Romidepsin(Synonyms: 罗米地辛; FK 228; FR 901228; NSC 630176)

    Romidepsin Chemical Structure

    CAS No. : 128517-07-7

    规格 价格 是否有货 数量
    1 mg ￥1000 In-stock
    5 mg ￥2900 In-stock
    10 mg ￥4950 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    Romidepsin 相关产品

    •相关化合物库:

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

    生物活性

    Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively[1]. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis[2].

    IC50 & Target[1]

    HDAC1

    36 nM (IC50)

    HDAC2

    47 nM (IC50)

    HDAC4

    510 nM (IC50)

    HDAC6

    14000 nM (IC50)

    体外研究
    (In Vitro)

    Romidepsin (0-72 hours; 0-80 nM) inhibits proliferation of HCC cells in dose-dependent manner[2].
    Romidepsin (0-48 hours; 0-60 nM) leads to a time- and dose-dependent induction of cell cycle arrest in the G2/M phase in HCC cells[2].
    Romidepsin (0-48 hours; 0-60 nM) promotesapoptosis in HCC cells, increases c-caspase-3, c-caspase-9, and c-PARP protein expression[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.

    Cell Proliferation Assay[2]

    Cell Line: HCC cells
    Concentration: 0 nM; 10 nM; 20 nM; 30 nM; 40 nM; 50 nM; 60 nM; 70 nM; 80 nM
    Incubation Time: 0 hours; 12 hours; 24 hours; 48 hours; 72 hours
    Result: Inhibited HCC cells proliferation.

    Cell Cycle Analysis[2]

    Cell Line: HCC cells
    Concentration: 0 nM; 15 nM; 30 nM; 60 nM
    Incubation Time: 12 hours;24 hours; 48 hours
    Result: Caused a G2/M arrest.

    Western Blot Analysis[2]

    Cell Line: HCC cells
    Concentration: 0 nM; 15 nM; 30 nM; 60 nM
    Incubation Time: 12 hours;24 hours; 48 hours
    Result: Increaesd c-caspase-3, c-caspase-9, and c-PARP expression in HCC cells.

    体内研究
    (In Vivo)

    Romidepsin (intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days) inhibited the tumor growth, reveals a higher expression of p-cdc25C, ki67, c-caspase-3 and c-PARP, and a lower expression of Ki-67 in Romidepsin treated tumors [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: Nude mice with Huh7 cells[2]
    Dosage: 0.5 and 1 mg/kg
    Administration: Intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days
    Result: Suppressed tumor growth in mouse xenograft models.

    Clinical Trial

    分子量

    540.70

    Formula

    C24H36N4O6S2
    CAS 号

    128517-07-7
    中文名称

    罗米地辛
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 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: 

    DMSO : ≥ 100 mg/mL (184.95 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 1.8495 mL 9.2473 mL 18.4945 mL
    5 mM 0.3699 mL 1.8495 mL 3.6989 mL
    10 mM 0.1849 mL 0.9247 mL 1.8495 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: ≥ 2.08 mg/mL (3.85 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (3.85 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 (3.85 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.08 mg/mL (3.85 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 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 (3.85 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (3.85 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]. Furumai R, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 Sep 1;62(17):4916-21.

      [2]. Sun WJ, et al. Romidepsin induces G2/M phase arrest via Erk/cdc25C/cdc2/cyclinB pathway and apoptosis induction through JNK/c-Jun/caspase3 pathway in hepatocellular carcinoma cells. Biochem Pharmacol. 2017 Mar 1;127:90-100.

    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

    德国KGW搅拌器型杜瓦瓶11621/11626/11622-S/11627-S

    发表于由

    【简单介绍】

    德国KGW搅拌器型杜瓦瓶11621/11626/11622-S/11627-S，紧凑型设计，银色外壳；适合混合储存使用-200-+200℃的介质；可以配套选择WIGGENS各种搅拌子；可以配套WIGGENS磁力搅拌器使用。

    【详细说明】

    德国KGW搅拌器型杜瓦瓶11621/11626/11622-S/11627-S

    主要特点：

    德国KGW搅拌器型杜瓦瓶11621/11626/11622-S/11627-S

    1. 适合混合储存使用-200-+200℃的介质
    2. 紧凑型设计，银色外壳
    3. 可以配套选择WIGGENS各种搅拌子
    4. 可以配套WIGGENS磁力搅拌器使用



    订货信息：

    订货号 型号

    内容积

    mL

    内径/内高

    mm
    11621 MRD1-E 550 85 / 100
    11622-S MRD2S-E 2300 138 / 160
    11626 MRT1-E 550 85 / 100
    11627-S MRT2S-E 2300 138 / 160

    德国KGW搅拌器型杜瓦瓶MRD1-E/MRD2S-E/MRT1-E/MRT2S-E

    液氮罐使用中的常见问题和注意事项！ 

    液氮是一种低温制品，在生物医学研究工作中，液氮是研究样品的主要冷冻贮存媒介。一些使用者在实际生产中，发现由于对液氮及液氮生物容器特性的不了解，而造成的不合理使用现象严重，既易造成液氮的浪费，增加生产成本，严重的还可能发生伤人事故。下面是一些常见问题： 
    一、液氮罐的种类：液氮罐一般可分为贮存罐、运输罐两种。贮存罐主要用于室内液氮的静置贮存，不宜在工作状态下作远距离运输使用；运输罐为了满足运输的条件，作了专门的防震设计。其除可静置贮存外，还可在充装液氮状态下，作运输使用，但也应避免剧烈的碰撞和震动
    二、液氮罐口不能密封液氮贮存在液氮罐中时，要注意将液氮罐口保留一定缝隙，否则由于液氮气化时气体无法及时排出，极易造成爆炸事故发生。一般液氮罐的盖塞都留有一定的缝隙，在使用时千万不要人为的将其堵塞。
    三、液氮使用注意事项
    1、液氮是低温制品，在使用过程中要防止冻伤 
    2、在液氮中操作及存取冷冻物品时速度要快，要注意轻拿轻放，以免内容物解冻，造成不必要的损失。
    3、在使用和贮存液氮的房间内，要保持通风良好，以避免空间缺氧，造成窒息。
    4、由于液氮不具杀菌性，故接触液氮的用具要注意消毒。
    5、液氮罐在运输过程中一定要固定好，以防震动和倒翻。
    四、液氮罐内液氮的贮存使用液氮罐贮存物品时，要注意及时补充液氮。液氮液面以不低于冷藏物品为宜。检查液氮贮存量时，可使用称重法或手电筒照射法，亦可用细木、竹竿插入液氮罐中视其结霜高度（等于液面高度）的方法。但切勿用空心管插入，以免液氮从管内冲出飞溅伤人。
    一般液氮罐使用一年后，要清洗消毒一次。清洗时要先用中性洗涤剂洗刷，再用不高于40℃的温水冲洗干净，待内胆充分干燥后，才可再充装液氮。 

    光翠雀碱对照品

    发表于由
    光翠雀碱对照品

      【编号】：PR0481

      【产品名称】：光翠雀碱对照品

      【规格】：10mg

      【用途】：

    　　光翠雀碱对照品

    　　编号：PR0481
    　　英文名称：Denudatine
    　　Cas 号: 26166-37-0
    　　分 子 式：C22H33NO2
    　　分 子 量：343.511
    　　植物来源：附子,乌头
    　　来源: Alkaloid from Root of Delphinium denudatum. Also Aconitum jinyangense (Ranunculaceae)
    　　纯度: 95%~99%
    　　分析方法: HPLC-DAD or/and HPLC-ELSD
    　　鉴定方法: 质谱（Mass）, 核磁（NMR）
    　　包装: 棕色小玻璃瓶，标准包装10mg，20mg，50mg；可以按客户需求包装。
    　　类别：上海金畔生物科技有限公司，天然提取物
    　　作为标准品，对照品或者供研究用，不能直接用于人体。

    PTP1B-IN-3

    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。

    PTP1B-IN-3 

    PTP1B-IN-3 是有效的，有选择性的 PTP1B 抑制剂，对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 具有抗糖尿病和抗癌作用。

    PTP1B-IN-3

    PTP1B-IN-3 Chemical Structure

    CAS No. : 809272-64-8

    规格 价格 是否有货
    1 mg ￥8500 询问价格 & 货期
    5 mg ￥25000 询问价格 & 货期
    10 mg ￥44000 询问价格 & 货期

    * Please select Quantity before adding items.

    PTP1B-IN-3 的其他形式现货产品:

    PTP1B-IN-3 diammonium

    生物活性

    PTP1B-IN-3 is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 has antidiabetic and anticancer effects[1][2].

    IC50 & Target

    IC50: 120 nM (PTP1B), 120 nM (TCPTP) [2]
    体内研究
    (In Vivo)

    In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits dose dependent inhibition (60%, 80% and 100% inhibition at 1, 3 and 10 mg/kg, respectively) of glucose excursion when given orally 2 h before oral glucose challenge with an estimated ED50 of 0.8 mg/kg[1].
    In the NDL2 Ptpn1 transgenic mice, PTP1B-IN-3 (compounds 3g; orally; 30 mg/kg for 21 days) shows a significant delay in the onset of tumor development in NDL2 Ptpn1+/+ mice, extending the median tumor free days (T50) from 28 days to 75 days[1].
    In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits good oral bioavailability (F of 24%), slow clearance (CL of 0.71 mL/kg/min), and good elimination half live (t1/2 of 6 h). The oral bioavailability in higher species such as rats (F of 4%) and squirrel monkeys (F of 2%) are substantially lower but excellent exposures are achieved with oral dosing[1].

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

    362.06

    Formula

    C12H7BrF2NO3P
    CAS 号

    809272-64-8
    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]. Yongxin Han, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5.

      [2]. Patel D, .Discovery of orally active, potent, and selective benzotriazole-based PTP1B inhibitors. ChemMedChem. 2011 Jun 6; 6(6):1011-6.

    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

    Lenalidomide(Synonyms: 来那度胺; CC-5013)

    发表于由

    Lenalidomide (Synonyms: 来那度胺; CC-5013) 纯度: 99.86%

    Lenalidomide (CC-5013) 是 Thalidomide 的衍生物，也是一种具有口服活性免疫调节剂，以分子胶的方式作用。Lenalidomide (CC-5013) 是一种泛素 E3 连接酶 cereblon (CRBN) 的配体，可通过 CRBN-CRL4 泛素连接酶对两种淋巴转录因子 IKZF1 和 IKZF3 进行选择性泛素化和降解。Lenalidomide (CC-5013) 特别地抑制成熟 B 细胞淋巴瘤 (包括多发性骨髓瘤) 的生长，并诱导 T 细胞释放白细胞介素-2 (IL-2)。

    Lenalidomide(Synonyms: 来那度胺; CC-5013)

    Lenalidomide Chemical Structure

    CAS No. : 191732-72-6

    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 ￥1045 In-stock
    50 mg ￥950 In-stock
    100 mg ￥1350 In-stock
    500 mg ￥2200 In-stock
    1 g ￥3600 In-stock
    5 g   询价  
    10 g   询价  

    * Please select Quantity before adding items.

    Lenalidomide 相关产品

    •相关化合物库:

    • Drug Repurposing Compound Library Plus
    • FDA-Approved Drug Library Plus
    • FDA-Approved Drug Library Mini
    • Bioactive Compound Library Plus
    • Apoptosis Compound Library
    • Immunology/Inflammation Compound Library
    • FDA-Approved Drug Library
    • Anti-Cancer Compound Library
    • CNS-Penetrant Compound Library
    • Drug Repurposing Compound Library
    • Ubiquitination Compound Library
    • Anti-COVID-19 Compound Library
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    • Orally Active Compound Library
    • FDA Approved & Pharmacopeial Drug Library
    • Drug-Induced Liver Injury (DILI) Compound Library
    • Anti-Blood Cancer Compound Library
    • Transcription Factor Targeted Library
    • Rare Diseases Drug Library

    生物活性

    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].

    IC50 & Target[5]

    Cereblon

     

    体外研究
    (In Vitro)

    Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells[2]. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC50 values of ~30 μM, ~3 μM and ~3 μM, respectively, These reduced CRBN expression cells (U266-CRBN60 and U266-CRBN75) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10 μM[3]. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation[5].

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

    The toxicity of Lenalidomide doses up to 15, 22.5, and 45 mg/kg via IV, IP, and PO routes of administration. Limited by solubility in our PBS dosing vehicle, these maximum achievable Lenalidomide doses are well tolerated with the exception of one mouse death (of four total dosed) at the 15 mg/kg IV dose. Notably, no other toxicities are observed in the study at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45) or at any other dose level through IV, IP, and PO routes[4].

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

    分子量

    259.26

    Formula

    C13H13N3O3
    CAS 号

    191732-72-6
    中文名称

    来那度胺；雷那度胺
    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 (385.71 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.8571 mL 19.2857 mL 38.5713 mL
    5 mM 0.7714 mL 3.8571 mL 7.7143 mL
    10 mM 0.3857 mL 1.9286 mL 3.8571 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 (9.64 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (9.64 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 (9.64 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (9.64 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 (9.64 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (9.64 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 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 MCE 网站选购。
    参考文献

    • [1]. Krönke J, et al. Lenalidomide induces degradation of IKZF1 and IKZF3. Oncoimmunology. 2014 Jul 3;3(7):e941742.

      [2]. Kotla V, et al. Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36.

      [3]. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35.

      [4]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82.

      [5]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.

      [6]. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.

      [7]. Omran A, et al. Effects of MRP8, LPS, and lenalidomide on the expressions of TNF-α , brain-enriched, and inflammation-related microRNAs in the primary astrocyte culture. ScientificWorldJournal. 2013 Sep 21;2013:208309.
    Cell Assay
    [3]

    Cell lines NCI-H929 and U266, and DF15 cells are grown in RPMI-I640 medium containing 10% (V/V) heat-inactivated fetal bovine serum supplemented with 2 mM glutamine. To produce Lenalidomide resistant cell lines, NCI-H929 cells are treated continuously (fresh Lenalidomide is added every 3-4 days) with control (final 0.1% DMSO) or low-dose Lenalidomide (1 μM) for 2 months until the proliferation of cells is no longer inhibited by Lenalidomide (1 μM), as determined by cell viability (Vi-cell XR cell viability analyzer), cell proliferation by flow cytometry and cell cycle analysis (propidium iodide staining). After acquisition of resistance to 1 μM, the resistant H929 cell lines are treated with Lenalidomide (10 μM) for a further 4 months. After this period of time, the cell cultures achieved fully establish resistance up to high-dose Lenalidomide (30 μM). Prior to the experiments described here, H929 Lenalidomide-resistant cells are taken out of culture with compounds for 5-7 days before use[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice[4]
    Imprinting control region (ICR) mice 8-10 weeks of age are used. Lenalidomide is incompletely soluble at 3.5 mg/mL and above in PBS containing 1% HCl, as visible particulates remained after thorough mixing. Therefore 3 mg/mL is selected as the maximum dosing solution concentration (with no visible particulates). Single, individual mice are initially dosed with 3, 10, or 15 mg/kg IV; 4.5, 15, or 22.5 mg/kg IP; and 9, 30, or 45 mg/kg PO. Additional mice (n=4) are then evaluated at the maximum dose achievable by volume and solubility of Lenalidomide in the dosing solution. All mice are monitored closely for 1 h and re-evaluated for toxicities 3, 6, and 24 h postdose[4].

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

    • [1]. Krönke J, et al. Lenalidomide induces degradation of IKZF1 and IKZF3. Oncoimmunology. 2014 Jul 3;3(7):e941742.

      [2]. Kotla V, et al. Mechanism of action of lenalidomide in hematological malignancies. J Hematol Oncol. 2009 Aug 12;2:36.

      [3]. Lopez-Girona A, et al. Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. Leukemia. 2012 Nov;26(11):2326-35.

      [4]. Rozewski DM, et al. Pharmacokinetics and tissue disposition of lenalidomide in mice. AAPS J. 2012 Dec;14(4):872-82.

      [5]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.

      [6]. Nagashima, Takeyuki, et al. PHARMACEUTICAL COMPOSITION COMPRISING BICYCLIC NITROGEN-CONTAINING AROMATIC HETEROCYCLIC AMIDE COMPOUND AS ACTIVE INGREDIENT. Patent. 20170360780A1.

      [7]. Omran A, et al. Effects of MRP8, LPS, and lenalidomide on the expressions of TNF-α , brain-enriched, and inflammation-related microRNAs in the primary astrocyte culture. ScientificWorldJournal. 2013 Sep 21;2013:208309.

    LJH685

    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。

    LJH685  纯度: 98.08%

    LJH685 是一种有效的选择性，ATP-竞争性的 RSK 抑制剂, 抑制 RSK1/2/3 生物活性, IC50 为 6、5、4 nM。

    LJH685

    LJH685 Chemical Structure

    CAS No. : 1627710-50-2

    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 ￥1045 In-stock
    5 mg ￥950 In-stock
    10 mg ￥1600 In-stock
    50 mg ￥6000 In-stock
    100 mg ￥11000 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    LJH685 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus
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    • Kinase Inhibitor Library
    • MAPK Compound Library
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    • Oxygen Sensing Compound Library
    • Glutamine Metabolism Compound Library
    • Anti-Cancer Metabolism Compound Library

    生物活性

    LJH685 is a potent, ATP-competitive and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50s of 6, 5, 4 nM, respectively[1].

    IC50 & Target

    IC50: 6 nM (RSK1), 5 nM (RSK1), 4 nM (RSK1)[1]
    体外研究
    (In Vitro)

    LJH685 (0.01-100 μM; 72 hours) efficiently inhibits the growth of MDA-MB-231 and H358 cells in soft agar with EC50s of 0.73 and 0.79 μM, respectively[1].
    LJH685 (0.1-10 μM; 4 hours) efficiently reduces phosphorylation of YB1 at submicromolar concentrations and causes nearly complete inhibition at higher concentrations[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 Proliferation Assay[1]

    Cell Line: MDA-MB-231, H358 cells
    Concentration: 0.01, 0.1, 1, 10, 100 μM
    Incubation Time: 72 hours
    Result: The growth in soft agar was efficiently inhibited with EC50 values of 0.73 and 0.79 μM in MDA-MB-231 and H358, respectively.

    Western Blot Analysis[1]

    Cell Line: MDA-MB-231, H358 cells
    Concentration: 0.1, 0.3, 1, 3, 10 μM
    Incubation Time: 4 hours
    Result: Efficiently reduced phosphorylation of YB1 at submicromolar concentrations and caused nearly complete inhibition at higher concentrations.

    分子量

    381.42

    Formula

    C22H21F2N3O
    CAS 号

    1627710-50-2
    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 : ≥ 31 mg/mL (81.28 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 2.6218 mL 13.1089 mL 26.2178 mL
    5 mM 0.5244 mL 2.6218 mL 5.2436 mL
    10 mM 0.2622 mL 1.3109 mL 2.6218 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 mg/mL (2.62 mM); Clear solution

      此方案可获得 ≥ 1 mg/mL (2.62 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (2.62 mM); Clear solution

      此方案可获得 ≥ 1 mg/mL (2.62 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 10.0 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: ≥ 1 mg/mL (2.62 mM); Clear solution

      此方案可获得 ≥ 1 mg/mL (2.62 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 10.0 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]. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12.

      [2]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015 Aug 21;6(24):20570-7.

      [3]. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.

      [4]. My-My Huynh, et al. RSK2: a promising therapeutic target for the treatment of triple-negative breast cancer. Expert Opin Ther Targets. 2020 Jan;24(1):1-5.

    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

    郑州长城科工贸超低温循环冷却器LT-100-80

    发表于由

    郑州长城科工贸超低温循环冷却器LT-100-80

  • 品牌 长城科工贸|Greatwall
  • 型号 LT-100-80
  • 商品详情

    主要用于为需冷设备提供超低温循环冷却液体，维持在低温条件下工作的低温反应;可与20L、50L、100L等反应釜配套使用，将反应釜内物料冷却到-70℃、-80℃、-100℃。

    ● 采用微机控制，全数字化中文显示，操作方便。温度显示采用高亮度LED。高低压保护、过载保护、过电流保护功能。

    ● 环保无氟制冷剂，符合欧盟及国家标准。

    ● 制冷系统压缩机、油分离器、电磁阀、膨胀阀等均采用进口品牌。

    ● 蒸发器为全钎焊板式换热器。

    ● 耐低温专用循环泵，低温工况下无泄漏、无堵转现象。

    ● 循环系统采用密闭式循环系统。无挥发保护实验人员健康。

    ● 储液槽及载冷介质全部采用304不锈钢材质，耐腐蚀性好。

    ● 整机稳定可靠，能满足24h以上连续生产对工艺冷源的需求。

    ● 主机冷却方式为风冷。

    ● 外壳为静电喷塑SPCC，防腐效果好。

    型号

    LT-20-80

    LT-50-80

    LT-100-80

    LT-100-110

       使用温度范围（℃）

    -80~-40

    -80~-40

    -80~-40

    -100~-60

       温度稳定性（℃）

    ±2

    ±2

    ±2

    ±2

       最佳环境温度（℃）

    5~25

    5~25

    5~25

    5~25

       电源（V/Hz）

    3~，380V，50Hz

    3~，380V，50Hz

    3~，380V，50Hz

    3~，380V，50Hz

       整机功率（kW）

    4.9

    9.8

    19.3

    38

       制冷剂

    R404A/R23

    R404A/R23

    R404A/R23

    R404A/R23/R14

    制冷量（W）

    -40℃

    2000

    5000

    10000

    –

    -60℃

    1400

    3000

    6000

    –

    -80℃

    450

    1000

    2500

    5500

    -90℃

    –

    –

    –

    3700

    -100℃

    –

    –

    –

    2500

    循环泵

    功率（W）

    280

    280

    280

    2800

    额定流量（L/min）

    30

    30

    30

    50

    压力（bar）

    1.0

    1.0

    1.0

    3.0

    储液槽容积（L）

    10

    10

    24

    100

    外形尺寸（mm）

    1060D×645W×1320H

    1200L×710W×1280H

    1435D×850W×1598H

    2950L×1500W×2385H

       重量（kg）

    235

    350

    600

    1500

    • Birinapant(Synonyms: 比瑞那帕; TL32711)

    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。

    Birinapant (Synonyms: 比瑞那帕; TL32711) 纯度: 99.70%

    Birinapant (TL32711) 是一种二价 Smac 模拟物，是 XIAP 和 cIAP1 的强效拮抗剂，Kd 值分别为 45 nM 和小于 1 nM。Birinapant (TL32711) 诱导完整细胞中 cIAP1 和 cIAP2 的自身泛素化和蛋白酶体降解，从而形成 RIPK1: caspase-8 复合物，caspase-8 活化和诱导肿瘤细胞死亡。Birinapant (TL32711) 靶向与 TRAF2 相关的 cIAP，并消除 TNF 诱导的 NF-κB 活化。

    Birinapant(Synonyms: 比瑞那帕; TL32711)

    Birinapant Chemical Structure

    CAS No. : 1260251-31-7

    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 ￥1953 In-stock
    2 mg ￥850 In-stock
    5 mg ￥1400 In-stock
    10 mg ￥2200 In-stock
    50 mg ￥6500 In-stock
    100 mg ￥9950 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    Birinapant 相关产品

    •相关化合物库:

    • Drug Repurposing Compound Library Plus
    • Clinical Compound Library Plus
    • Bioactive Compound Library Plus
    • Anti-Infection Compound Library
    • Apoptosis Compound Library
    • NF-κB Signaling Compound Library
    • Anti-Cancer Compound Library
    • Clinical Compound Library
    • Antiviral Compound Library
    • Peptidomimetic Library
    • Drug Repurposing Compound Library
    • Anti-COVID-19 Compound Library

    生物活性

    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

    IC50 & Target

    Kd: 45 nM (XIAP), <1 nm (ciap1)[1]
    体外研究
    (In Vitro)

    Birinapant (TL32711) (30-10000 nM; 24 hours) significantly decreases the viability of SUM190 cells in a dose-dependent manner[1].
    Birinapant (TL32711) (30-1000 nM; 4 hours) shows a significant decrease in cIAP1 levels and enhanced PARP cleavage, and induces apoptosis[1].
    Birinapant (TL32711) binds with high affinity to the isolated BIR3 domains of cIAP1, cIAP2, and XIAP and the single BIR domain of ML-IAP and rapidly degrades TRAF2-bound cIAP1 and cIAP2 thereby inhibiting TNF-mediated NF-κB activation[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: TRAIL-resistant SUM190 IBC cells
    Concentration: 30, 100, 300, 1000, 10000 nM
    Incubation Time: 24 hours
    Result: Significantly decreased the viability of SUM190 cells in a dose-dependent manner.

    Western Blot Analysis[1]

    Cell Line: SUM190 cells
    Concentration: 30, 300, 1000 nM
    Incubation Time: 4 hours
    Result: Showed a significant decrease in cIAP1 levels and enhanced PARP cleavage.

    体内研究
    (In Vivo)

    Birinapant (TL32711) (30 mg/kg; i.p.; every third day (*5)) shows antitumor efficacy and are devoid of overt toxicity in preclinical models[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: Female athymic nude mice (low-passage, patient-derived xenotransplant models of ovarian cancer, colorectal cancer, and melanoma)[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; every third day (*5)
    Result: Resulted in inhibition of tumor growth.

    Clinical Trial

    分子量

    806.94

    Formula

    C42H56F2N8O6
    CAS 号

    1260251-31-7
    中文名称

    比瑞那帕
    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 : 125 mg/mL (154.91 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.2392 mL 6.1962 mL 12.3925 mL
    5 mM 0.2478 mL 1.2392 mL 2.4785 mL
    10 mM 0.1239 mL 0.6196 mL 1.2392 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: ≥ 2.08 mg/mL (2.58 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (2.58 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 (2.58 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.08 mg/mL (2.58 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 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 (2.58 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (2.58 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]. Allensworth JL, et al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism. Breast Cancer Res Treat. 2013 Jan;137(2):359-71.

      [2]. Krepler C, et al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94.

      [3]. Nguyen QD, et al. Temporal and spatial evolution of therapy-induced tumor apoptosis detected by caspase-3-selective molecular imaging. Clin Cancer Res. 2013 Jul 15;19(14):3914-24.

      [4]. Benetatos CA, et al. Birinapant (TL32711), a bivalent SMAC mimetic, targets TRAF2-associated cIAPs, abrogates TNF-induced NF-κB activation, and is active in patient-derived xenograft models. Mol Cancer Ther. 2014 Apr;13(4):867-79.

    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

    单点挂壁式气体检测仪TN-50

    发表于由

    【简单介绍】

    单点挂壁式气体检测仪TN-50 主要应用冶金、化工、石油、制药、环保等行业工作环境存在有毒、有害气体或氧气含量的监测，而又不需要防爆的场所。检测仪采用进口电化学传感器（可燃气是催化燃烧式），精度高、反应灵敏，抗干扰能力强、使用寿命长。现场LED显示，声光报警。智能化设计，操作简单，校准、调零、报警设置方便。可输出继电器控制信号。采用AC220V供电。

    【详细说明】

    单点挂壁式气体检测仪TN-50

    产品概述： 

    传感器类型：电化学（可燃气使用催化燃烧式，特殊的另行说明）

    响应时间：≤40s

    工作模式：连续工作，可设置高低报警点

    模拟接口：4-20mA输出【选配】

    数字接口：RS485总线接口【选配】

    后备电源：提供超过12小时的断电续航能力【选配】

              提供电池状态指示灯

    显示方式：图形液晶显示，直观方便

    报警方式：声音报警 —  90dB以上（10cm）

    单点挂壁式气体检测仪TN-50

              光 报 警 — 高亮度频闪灯

    输出控制：两路报警控制的继电器输出

    附加功能：时间、日历显示

    工作电压：AC220V/50Hz

    防水防尘：IP65

    使用环境：温度－20℃ ～ 50℃

              湿度10 ～ 90％（RH）无冷凝

    安装方式：壁挂式安装

    外形尺寸：230mm×150mm×75mm

    重    量：1800g

    订货信息：