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BAY-1436032

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。

BAY-1436032  纯度: 99.09%

BAY-1436032 是一种新型的泛突变异柠檬酸脱氢酶 1 (IDH1) 抑制剂。

BAY-1436032

BAY-1436032 Chemical Structure

CAS No. : 1803274-65-8

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 ¥1510 In-stock
5 mg ¥1400 In-stock
10 mg ¥2300 In-stock
25 mg ¥4600 In-stock
50 mg ¥7500 In-stock
100 mg ¥11500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

BAY-1436032 相关产品

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  • Anti-Cancer Metabolism Compound Library
  • Mitochondria-Targeted Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

IC50 & Target

IDH1[1]

体外研究
(In Vitro)

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor. BAY-1436032 inhibits intracellular (R)-2-hydroxyglutarate (R-2HG) production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C with IC50s of 60 and 45 nM, respectively. R-2HG levels are not reduced in IDH2R140Q and IDH2R172K expressing mouse hematopoietic cells by BAY-1436032 at concentrations up to 10 μM. Colony growth is inhibited by 50% at a concentration of 0.1 μM BAY-1436032, while concentrations up to 100 μM do not suppress colony growth of patient-derived IDH1 wild-type AML cells. On morphologic evaluation myelomonocytic differentiation of myeloid progenitors is strongly induced by BAY-1436032[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)

Long-term exposure to once daily oral BAY-1436032 reveals nearly complete suppression of (R)-2-hydroxyglutarate (R-2HG) production with 150 mg/kg BAY1436032. White blood cell counts constantly increase in vehicle-treated mice and, at a lower rate, in animals receiving 45 mg/kg BAY-1436032, while they remain constant in the 150 mg/kg cohort. Hemoglobin levels are slightly lower in the vehicle and 45 mg/kg groups as compare to the 150 mg/kg cohort at day 60, while platelet counts are significantly reduced in vehicle and 45 mg/kg BAY-1436032 treated mice compare to the 150 mg/kg cohort at day 60. All mice receiving 150 mg/kg BAY-1436032 survive with minimal hCD45+ cell load in their peripheral blood until the end of observation at day 150 after treatment start (P<0.001), while vehicle-treated animals die from leukemia with a median survival of 91 days. Mice treated with 45 mg/kg BAY-1436032 display intermediate levels of CD14/CD15 expression[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

489.53

Formula

C26H30F3N3O3

CAS 号

1803274-65-8

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 (255.35 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0428 mL 10.2139 mL 20.4278 mL
5 mM 0.4086 mL 2.0428 mL 4.0856 mL
10 mM 0.2043 mL 1.0214 mL 2.0428 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 (5.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.11 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 (5.11 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.11 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 (5.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.11 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]. Chaturvedi A, et al. Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo. Leukemia. 2017 Oct;31(10):2020-2028.

Cell Assay
[1]

Colony-forming cell (CFC) units are assayed in methylcellulose supplemented with 10 ng/mL IL-3, 10 ng/mL GM-CSF, 50 ng/ mL SCF, 50 ng/mL FLT3-ligand and 3 U/mL EPO. Vehicle or BAY-1436032 is added to methylcellulose containing 105 human mononuclear cells, which are plated in duplicate. Colonies are evaluated microscopically 10 to 14 days after plating by standard criteria[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]

NSG mice are used and transplanted with primary acute myeloid leukemia (AML) cells from a patient with IDH1R132C mutant AML. Per condition 10 mice are treated with vehicle, 45 or 150 mg/kg body weight BAY-1436032 once daily by oral gavage for 150 days starting 17 days after transplantation. Finally, serum R-2HG levels and human CD45+ (hCD45+) cells are measured[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]. Chaturvedi A, et al. Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo. Leukemia. 2017 Oct;31(10):2020-2028.

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Maleic hydrazide(Synonyms: 抑芽丹;马来酰肼;青鲜素)

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。

Maleic hydrazide (Synonyms: 抑芽丹;马来酰肼;青鲜素) 纯度: 99.91%

Maleic hydrazide广泛用作植物生长调节剂和除草剂。Maleic hydrazide 是核酸和蛋白质合成的抑制剂。

Maleic hydrazide(Synonyms: 抑芽丹;马来酰肼;青鲜素)

Maleic hydrazide Chemical Structure

CAS No. : 123-33-1

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 ¥610 In-stock
500 mg ¥550 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Maleic hydrazide 相关产品

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  • Anti-Aging Compound Library

生物活性

Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins[1][2].

体外研究
(In Vitro)

Maleic hydrazide is used in agriculture-in despite its known effect as a mutagenic and clastogenic agent. Maleic hydrazide had lower IC50 values for all cell lines compared to Ethephon. Maleic hydrazide also showed least cytotoxicity on Vero cells, followed by Hep2 and HepG2 cells[3].

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

体内研究
(In Vivo)

Maleic hydrazide has a low acute toxicity by oral, dermal, and inhalation routes of exposure[3].

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

分子量

112.09

Formula

C4H4N2O2

CAS 号

123-33-1

中文名称

抑芽丹;马来酰肼;青鲜素

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 (1115.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 8.9214 mL 44.6070 mL 89.2140 mL
5 mM 1.7843 mL 8.9214 mL 17.8428 mL
10 mM 0.8921 mL 4.4607 mL 8.9214 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 (18.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (18.56 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (18.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (18.56 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

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

    Solubility: ≥ 2.08 mg/mL (18.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (18.56 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Venezian A, et al. The Influence of the Plant Growth Regulator Maleic Hydrazide on Egyptian Broomrape Early Developmental Stages and Its Control Efficacy in Tomato under Greenhouse and Field Conditions. Front Plant Sci. 2017;8:691. Published 2017 May 16.

    [2]. Swietlińska Z, et al. Cytotoxic effects of maleic hydrazide. Mutat Res. 1978;55(1):15-30.

    [3]. Yurdakok B, et al. Cytotoxic effects of etephon and maleic hydrazide in Vero, Hep2, HepG2 cells. Drug Chem Toxicol. 2014;37(4):459-465.

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AZD5582

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。

AZD5582  纯度: 98.11%

AZD5582 是 IAP 拮抗剂,可以有效与 cIAP1,cIAP2 和 XIAP 的 BIR3 结构域结合, IC50 值分别为 15,21,15 nM。AZD5582 诱导凋亡 (apoptosis)。

AZD5582

AZD5582 Chemical Structure

CAS No. : 1258392-53-8

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 ¥1843 In-stock
2 mg ¥660 In-stock
5 mg ¥990 In-stock
10 mg ¥1800 In-stock
50 mg ¥5500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

AZD5582 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Peptidomimetic Library
  • Anti-Lung Cancer Compound Library

生物活性

AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis[1].

IC50 & Target[1]

cIAP1

15 nM (IC50)

cIAP2

21 nM (IC50)

XIAP

15 nM (IC50)

体外研究
(In Vitro)

AZD5582 (20 nM; 48 hours) inhibits cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells[2].
AZD5582 (20 nM; 17 or 25 hours) downregulates cIAP-1, activates RIPK1 (upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7[2].
AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells[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 Viability Assay[2]

Cell Line: H1975 NSCLC cell line
Concentration: 20 nM
Incubation Time: 48 hours
Result: Cooperated with IFNγ or viral double-stranded RNA (dsRNA) to inhibit cell viability even cell death.

Apoptosis Analysis[2]

Cell Line: HCC827 NSCLC cell line
Concentration: 20 nM
Incubation Time: 48 hours
Result: Had an inhibitory effect on cell viability by cooperating with IFNγ.

Western Blot Analysis[2]

Cell Line: H1975 NSCLC cell line
Concentration: 20 nM
Incubation Time: 17 or 25 hours
Result: Down-regulated cIAP-1, activated RIPK1 (upstream regulator of caspase-8), triggered the cleavage (activation) of caspase-3,7,8 and 9.

体内研究
(In Vivo)

AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved; when the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing 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: MDA-MB-231 xenograft-bearing mice[1]
Dosage: 0.1 mg/kg, 0.5 mg/kg, 3.0 mg/kg
Administration: Intravenous injection; once a week; 2 weeks
Result: Resulted in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg

分子量

1015.29

Formula

C58H78N8O8

CAS 号

1258392-53-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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 : ≥ 66.25 mg/mL (65.25 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9849 mL 4.9247 mL 9.8494 mL
5 mM 0.1970 mL 0.9849 mL 1.9699 mL
10 mM 0.0985 mL 0.4925 mL 0.9849 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: ≥ 2.5 mg/mL (2.46 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.46 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.46 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]. Hennessy EJ, et al. Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582). J Med Chem. 2013 Dec 27;56(24):9897-919.

    [2]. Qin Hao, et al. IF-γ and Smac mimetics synergize to induce apoptosis of lung cancer cells in a TNFα-independent manner,Cancer Cell Int. 2018; 18: 84.

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英国Stuart-SRT6滚轴混合仪器(模拟控制)

【简单介绍】

应用领域 其他 物料类型 其他
适用物料 其他 动力类型 其他
工作方式 其他

英国Stuart SRT6滚轴混合仪器(模拟控制)
– 模拟式SRT6型,以固定速度33rpm运行,用使用简便的开/关开关控制;用于搅拌血液样品, 粘性物质和液态-固态悬浮物,这些情况均要求Z低程度的气化。 本装置可用于高达60°C、湿度达80%的细菌培养箱中,或温度低到4°C的冷藏室中。

进口,质量保证!!

【详细说明】

英国Stuart SRT6滚轴混合仪器(模拟控制)

产品描述:

  英国Stuart SRT6滚轴混合仪器能提供柔和但高效、摇动起伏的作用。6根辊子的设计占空间很小。 以固定速度33rpm运行,用使用简便的开/关开关控制。

  用于搅拌血液样品, 粘性物质和液态-固态悬浮物,这些情况均要求低程度的气化。 本装置可用于高达60°C、湿度达80%的细菌培养箱中,或温度低到4°C的冷藏室中。 
两种滚动混合器均坚固耐用,设计结构容易清洁,有塑料辊子和滴液盘来收集意外的溢出物。

产品特点:

  1. 滚动和振动以便完全混合 
  2. 可选模拟速度控制或者数字速度控制 
  3. 六滚轴设计
  4. 连续静音运作设计 
  5. 可以在冷室或者培养箱内使用
    技术参数: 
产品编号 SRT6 SRT6D
控制方式 模拟控制,固定速度 数字控制,可变速度
滚轴数 6 6
速度 33rpm 5-60rpm
振幅 16mm 16mm
z大承载 10kg 10kg
滚轴规格 340×30mm 340×30mm
外部规格(宽×D×H) 565×240×110mm 565×240×110mm
净重 5.1kg 5.1kg
电源 230V/50Hz,50W 230V/50Hz,50W
IP等级 20 20

英国Stuart SRT6滚轴混合仪器(模拟控制)

订货信息:

产品型号 产品描述
SRT6 滚轴混合器,6个滚轴,模拟式控制,固定速度
SRT6D 滚轴混合器,6个滚轴,数字式控制,可变速度
SRT6ROLL 只有滚动作用,6个滚轴,模拟式控制,固定速度
SRT6DROLL 只有滚动作用,6个滚轴,数字式控制,可变速度

 

 

Tizaterkib(Synonyms: AZD0364)

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。

Tizaterkib (Synonyms: AZD0364) 纯度: 99.71%

Tizaterkib (AZD0364) 是一种有效的选择性 ERK2 抑制剂,IC50 为 0.6 nM。详细信息请参考专利文献 WO2017080979A1 中的化合物 example 18。

Tizaterkib(Synonyms: AZD0364)

Tizaterkib Chemical Structure

CAS No. : 2097416-76-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3080 In-stock
5 mg ¥2800 In-stock
10 mg ¥4800 In-stock
25 mg ¥9900 In-stock
50 mg 询价

* Please select Quantity before adding items.

Tizaterkib 相关产品

相关化合物库:

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  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

IC50 & Target[1]

ERK2

0.6 nM (IC50)

体外研究
(In Vitro)

Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib[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)

Tumor growth inhibition by Tizaterkib ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and Tizaterkib ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and Tizaterkib ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and Tizaterkib ethanesulfonic acid results in a reduction in tumor growth[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

494.50

Formula

C24H24F2N8O2

CAS 号

2097416-76-5

运输条件

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 100 mg/mL (202.22 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0222 mL 10.1112 mL 20.2224 mL
5 mM 0.4044 mL 2.0222 mL 4.0445 mL
10 mM 0.2022 mL 1.0111 mL 2.0222 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    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.21 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]. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

Cell Assay
[1]

KRAS-mutant Non-Small Cell Lung Cancer (NSCLC) A549, H2122, H2009, and Calu6 cell lines are seeded in 384-well black, clear bottomed plates, cultured for 18-24 hours and treated with increasing concentrations of AZD-0364 (7.143 nM, 61 nM, 357 nM, 2.143 μM and 10 μM) and Selumetinib (0-10 μM) in a 6×6 dosing matrix. Cells are seeded at a concentration such that cells in untreated wells are approximately 80% confluent at the end of the assay. After 3 days of treatment, live cell number is determined using a Sytox Green endpoint[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
A549 is a human non small cell lung cancer line carrying an oncogenic mutation in the KRAS gene (G12S). Female nude mice are implanted subcutaneously (s.c.) on the left flank, with 5×106 A549 cells (ATCC) per mouse.Tumor growth is monitored by twice weekly calliper measurement and volumes are calculated. Once tumors have reached a volume of ~200-300mm3 animals are randomised into groups of 7-11 and are treated with a continuous combination schedule of Selumetinib (ARRY-142886) 25 mg/kg BiD and AZD-0364 ethanesulfonic acid 25 mg/kg QD (four hours after first Selumetinib dose), both are dosed by peroral route. Tumor volumes are measured twice weekly after dosing commenced[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]. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.

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

Odoroside A

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。

Odoroside A  纯度: 98.75%

Odoroside A 是从夹竹桃叶中提取的一种有效成分。Odoroside A 具有抗癌活性。Odoroside A 通过 ROS/p53 信号通路诱导细胞凋亡和细胞周期阻滞,导致肿瘤细胞死亡。

Odoroside A

Odoroside A Chemical Structure

CAS No. : 12738-19-1

规格 价格 是否有货 数量
1 mg ¥2400 In-stock
5 mg ¥6500 In-stock
10 mg ¥9500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Odoroside A 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus

生物活性

Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death[1].

分子量

518.68

Formula

C30H46O7

CAS 号

12738-19-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

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

参考文献
  • [1]. Chen YY, et al. Proteomic Analysis Reveals that Odoroside A Triggers G2/M Arrest and Apoptosis in Colorectal Carcinoma Through ROS-p53 Pathway. Proteomics. 2019;19(15):e1900092.

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GW3965 hydrochloride

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

GW3965 hydrochloride  纯度: 99.73%

GW3965 hydrochloride 是肝 X 受体 (LXR) 激动剂,对 hLXRα 和 hLXRβ 的 EC50 分别为 190 nM 和 30 nM。

GW3965 hydrochloride

GW3965 hydrochloride Chemical Structure

CAS No. : 405911-17-3

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 ¥953 In-stock
5 mg ¥700 In-stock
10 mg ¥1000 In-stock
50 mg ¥3900 In-stock
100 mg ¥7400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GW3965 hydrochloride 相关产品

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  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Diabetes Related Compound Library
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  • Lipid Metabolism Compound Library
  • Targeted Diversity Library

生物活性

GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively[1][2][3].

IC50 & Target

EC50: 190 nM (hLXRα), 30 nM (hLXRβ)[4]

体外研究
(In Vitro)

GW3965 hydrochloride promotes GBM cell death in vitro with enhanced efficacy in EGFRvIII-expressing tumor cells. GW3965 hydrochloride up-regulates expression of the cholesterol transporter gene ABCA1 and the E3 ubiquitin ligase IDOL and reduces LDLR levels[2]. LXR ligands inhibits platelet aggregation and calcium mobilization stimulated by collagen or CRP. GW3965 hydrochloride (1 or 5 μM) displays a minor inhibitory effect on fibrinogen binding and P-selectin exposure, when platelets are stimulated with 1 μg/mL CRP. But using higher concentrations of GW3965 hydrochloride (10 μM) or T0901317 (40 μM), the levels of fibrinogen and P-selectin on the platelet surface are reduced[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)

GW3965 hydrochloride induces an increase of neuroactive steroids in the spinal cord, the cerebellum and the cerebral cortex of STZ-rats, but not in the CNS of non-pathological animals. GW3965 hydrochloride treatment induces an increase of dihydroprogesterone in the spinal cord of diabetic animals in association with an increase of myelin basic protein expression[1]. GW3965 hydrochloride (40 mg/kg, p.o.) strongly induces ABCA1 expression and reduces LDLR expression, and this is accompanied by 59% inhibition of tumor growth, and a 25-fold increase in GBM cell apoptosis in vivo[2]. GW3965 hydrochloride (2 mg/kg, i.v.) increases bleeding time and modulated platelet thrombus formation in vivo[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.

分子量

618.51

Formula

C33H32Cl2F3NO3

CAS 号

405911-17-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (161.68 mM; Need ultrasonic)

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6168 mL 8.0839 mL 16.1679 mL
5 mM 0.3234 mL 1.6168 mL 3.2336 mL
10 mM 0.1617 mL 0.8084 mL 1.6168 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: corn oil

    Solubility: 10 mg/mL (16.17 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 (4.04 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.04 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% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.04 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.04 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
  • 4.

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

    Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.04 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]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621.

    [2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456.

    [3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761.

    [4]. Collins JL, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem. 2002 May 9;45(10):1963-6.

Cell Assay
[2]

Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37ºC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.

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]

Diabetes is induced in two-month-old male rats by a single i.p. injection of freshly prepared STZ (65 mg/kg) in 0.09 M citrate buffer, pH 4.8. Control animals are injected with 0.09 mol/L citrate buffer at pH 4.8. Hyperglycemia is confirmed 48 h after streptozotocin injection by measuring tail vein blood glucose levels using a glucometer OneTouch Ultra2. Only animals with mean plasma glucose levels over 300 mg/mL are classified as diabetic. Glycemia is also assessed before treatment with Ro5-4864 or GW3965 hydrochloride and before death. Two months after STZ injection, diabetic animals are treated once a week with Ro5-4864 (3 mg/kg) or GW3965 hydrochloride (50 mg/kg). Thus, they receive four subcutaneous injections in a month. Control diabetic rats receive 200 μL of vehicle (sesame oil). Four-month-old non-diabetic male rats are injected, following the same experimental schedule, with Ro5-4864, GW3965 hydrochloride or vehicle. Rats are killed 24 h after the last treatment.

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]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621.

    [2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456.

    [3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761.

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