标签归档：vx

AVN-944(Synonyms: VX-944)

发表于由
回复

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。

AVN-944 (Synonyms: VX-944) 纯度: 99.56%

AVN-944(VX-944)是选择性非竞争性IMPDH抑制剂，对IMPDH1和IMPDH2的Ki值为6-10nMIMPDH。

AVN-944(Synonyms: VX-944)

AVN-944 Chemical Structure

CAS No. : 297730-17-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1786 In-stock
2 mg ￥1133 In-stock
5 mg ￥1700 In-stock
10 mg ￥2450 In-stock
50 mg ￥7500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

AVN-944 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • Targeted Diversity Library

生物活性

AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2. IC50 value: 6-10 nM (Ki) [1] Target: IMPDH in vitro: AVN-944 strikingly inhibit RNA synthesis within 2 h of exposure. Depletion of guanine nucleotides by MPA and AVN-944 also causes an early and near-complete reduction in levels of the 45S precursor rRNA synthesis and the concomitant translocation of nucleolar proteins including nucleolin, nucleophosmin, and nucleostemin from the nucleolus to the nucleoplasm [2]. AVN944 induced caspase-dependentand caspase-independent cell death in LNCaP, CWR22Rv1, and DU145 cells. AVN944 induced expression of p53-target proteins Bok, Bax and Noxa in androgen-responsive cell lines and suppressed expression of survivin in prostate cancer cells regardless of their androgen sensitivity. AVN944 also induced differentiation of androgen-independent prostate cancer cells as indicated by morphological changes and increased expression of genes coding for prostasomal proteins, keratins and other proteins, including tumor suppressor genes MIG-6 and NDRG1. AVN944-differentiated androgen-independent DU145 and PC-3 cells are sensitized to TRAIL-induced apoptosis as demonstrated by induction of caspases and PARP cleavage [3].

Clinical Trial

分子量

477.51

Formula

C25H27N5O5
CAS 号

297730-17-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (209.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.4710 mL 20.9420 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 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 (5.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.24 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 (5.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.24 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]. Zimmermann AG, et al. Inosine-5′-monophosphate dehydrogenase: regulation of expression and role in cellular proliferation and T lymphocyte activation. Prog Nucleic Acid Res Mol Biol. 1998;61:181-209.

    [2]. Huang M, et al. Guanine nucleotide depletion inhibits pre-ribosomal RNA synthesis and causes nucleolar disruption. Leuk Res. 2008 Jan;32(1):131-41.

    [3]. Floryk D, et al. Antiproliferative effects of AVN944, a novel inosine 5-monophosphate dehydrogenase inhibitor, in prostate cancer cells. Int J Cancer. 2008 Nov 15;123(10):2294-302.

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

VX-984(Synonyms: M9831)

发表于由
回复

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。

VX-984 (Synonyms: M9831) 纯度: 99.20%

VX-984 是一个有效的 DNA-PK 抑制剂。

VX-984(Synonyms: M9831)

VX-984 Chemical Structure

CAS No. : 1476074-39-1

规格 价格 是否有货 数量
5 mg ￥6500 In-stock
10 mg ￥11000 In-stock
50 mg ￥45000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

生物活性

VX-984 is a potent DNA-PK inhibitor.

Clinical Trial

分子量

415.49

Formula

C23H21D2N7O
CAS 号

1476074-39-1
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 : 10 mg/mL (24.07 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4068 mL 12.0340 mL 24.0680 mL
5 mM 0.4814 mL 2.4068 mL 4.8136 mL
10 mM 0.2407 mL 1.2034 mL 2.4068 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 (2.41 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.41 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% corn oil

    Solubility: ≥ 1 mg/mL (2.41 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.41 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]. By Charifson, Paul S; et al. DNA-PK inhibitors, US 20130281431 A1

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

Labnet VX-200型漩涡混合仪S0200-230V

发表于由

【简单介绍】

Labnet VX-200型漩涡混合仪S0200-230V有两种模式可供选择。接触模式（适合短时混合样品）和连续模式。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。其连续可调节速度使其适合于各种应用从温和的混合样品成悬浮状。VX-200漩涡混合仪身体娇小适合各种场所，适合在4 到65℃范围。

大量现货！
*中！

【详细说明】

Labnet VX-200型漩涡混合仪S0200-230V

 

产品简述：

    Labnet VX-200型漩涡混合仪S0200-230V的连续可调节速度使其适合于各种应用从温和的混合样品成悬浮状。大离心管，小离心管和酶标板等多种振荡板可供选择， 坚固的构造确保仪器的寿命期长，底座确保仪器不移动。VX-200漩涡混合仪身体娇小适合各种场所，适合在4 到65℃范围。

有两种模式可供选择。接触模式（适合短时混合样品）和连续模式。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。

 

技术特点

  1. 速度可连续任意变化控制
  2. 两种模式：接触式或连续操作式
  3. 大功率马达可对样品进行有效混合
  4. 适合在冷藏室或培养箱内使用
  5. 试管、离心管及酶标板等多种振荡板可供选择  

 

技术参数：

技术参数

 

速度：

0~2850rpm

操作模式：

接触式或连续操作

操作温度：

室温以上4～65°C

尺寸(长X宽X高) ：

14X16X13cm

重量：

2.2kg

电压及频率：

230V,50Hz

 

订货信息：

货号

详细信息

S0200-230V

VX-200漩涡混合器 标配CombiCup振荡板

S0200-21

24*1.5/2.0mL管，24*0.5mL和32*0.2mL管振荡板

S0200-22

一个微孔板或者64*0.2mL管或8*0.2mL八联管振荡板

S0200-23

8*15mL管或者8*12/13mm直径管振荡板

S0200-24

6*50mL管振荡板

S0200-25

12*1.5mL/2.0mL管振荡板，管水平放置

S0200-26

4*15mL管振荡板，管水平放置

S0200-27

5*50mL管振荡板，管水平放置

 

VX-200漩涡混合仪S0200-230V（标配振荡板）

发表于由

【简单介绍】

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

VX-200漩涡混合仪S0200-230V（标配振荡板）速度可连续调节，适合于各种应用从温和的混合样品成悬浮状。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。大离心管，小离心管和酶标板等多种振荡板可供选择，坚固的构造确保仪器的寿命期长，底座确保仪器不移动。

【详细说明】

VX-200漩涡混合仪S0200-230V（标配振荡板）

产品描述：

     VX-200漩涡混合仪S0200-230V（标配CombiCup振荡板），速度可连续调节，适合于各种应用从温和的混合样品成悬浮状。有两种模式可供选择。接触模式（适合短时混合样品）和连续模式。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。大离心管，小离心管和酶标板等多种振荡板可供选择，坚固的构造确保仪器的寿命期长，底座确保仪器不移动。VX-200漩涡混合仪身体娇小适合各种场所，适合在4到65℃范围。在空调房和温室都可以良好的使用。

技术特点

  • 两种模式：接触式或连续操作式
  • 速度可连续任意变化控制
  • 大功率马达可对样品进行有效混合
  • 适合在冷藏室或培养箱内使用 

技术参数：

型号 VX-200

速度

0~2850rpm

操作模式

接触式或连续操作

操作温度

室温以上4～65°C

尺寸(长X宽X高)

14X16X13cm

重量

2.2kg

电压及频率

230V,50Hz
货号 S0200-230V

订货信息

 

货号

详细信息

S0200-230V

VX-200漩涡混合器标配CombiCup振荡板

S0200-21

24*1.5/2.0mL管，24*0.5mL和32*0.2mL管振荡板

S0200-22

一个微孔板或者64*0.2mL管或8*0.2mL八联管振荡板

S0200-23

8*15mL管或者8*12/13mm直径管振荡板

S0200-24

6*50mL管振荡板

S0200-25

12*1.5mL/2.0mL管振荡板，管水平放置

S0200-26

4*15mL管振荡板，管水平放置

S0200-27

5*50mL管振荡板，管水平放置

VX-200漩涡混合仪S0200-230V（标配振荡板） 

VX-200涡旋混合仪器S0200-230V

发表于由

【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

美国Labnet VX-200涡旋混合仪器S0200-230V（标配CombiCup振荡板）适合于各种应用从温和的混合样品到悬浮样品。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。转头拆卸和互换都非常方便。大离心管，小离心管和酶标板等多种振荡板可供选择。
在空调房和温室都可以良好的使用。

【详细说明】

美国Labnet VX-200涡旋混合仪器S0200-230V（标配CombiCup振荡板）

产品简述：

  美国Labnet VX-200涡旋混合仪器S0200-230V可以在整个转速范围内真正实现漩涡震荡。连续可调节速度使VX-200漩涡混合仪适合于各种应用从温和的混合样品到悬浮样品。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。转头拆卸和互换都非常方便。大离心管，小离心管和酶标板等多种振荡板可供选择。坚固的构造确保仪器的寿命期长，底座确保仪器不移动。强力的驱动保证有效的震荡以及机器寿命。有两种模式可供选择，范围接触模式（适合短时混合样品）和连续模式。
VX-200漩涡混合仪在空调房和温室都可以良好的使用。

 

技术参数

型号名称 VX-200漩涡混合仪

转速：

0~2850rpm

操作运行模式：

接触式或连续操作

环境温度：

室温以上4～65°C

尺寸(长X宽X高) ：

14X16X13cm

重量：

2.2kg

电压及频率：

230V,50Hz

技术特点：

两种模式：接触式或连续操作式
大功率马达可对样品进行有效混合
速度可连续任意变化控制
试管、离心管及酶标板等多种振荡板可供选择
适合在冷藏室或培养箱内使用

订货信息：

货号

产品描述

S0200-230V

VX-200漩涡混合器 标配CombiCup振荡板

S0200-21

24*1.5/2.0mL管，24*0.5mL和32*0.2mL管振荡板

S0200-22

一个微孔板或者64*0.2mL管或8*0.2mL八联管振荡板

S0200-23

8*15mL管或者8*12/13mm直径管振荡板

S0200-24

6*50mL管振荡板

S0200-25

12*1.5mL/2.0mL管振荡板，管水平放置

S0200-26

4*15mL管振荡板，管水平放置

S0200-27

5*50mL管振荡板，管水平放置

Biricodar(Synonyms: VX-710)

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。

Biricodar (Synonyms: VX-710)

Biricodar (VX-710) 是 P-glycoprotein 和 MRP-1 的调节剂; 在多药耐药细胞中显示出有效的化学敏化活性。

Biricodar(Synonyms: VX-710)

Biricodar Chemical Structure

CAS No. : 159997-94-1

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

* Please select Quantity before adding items.

生物活性

Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.

体外研究
(In Vitro)

Biricodar shows activity against both P-glycoprotein (Pgp) and MRP-1 and also has activity in increasing drug uptake and retention and reversing drug resistance mediated by wild-type BCRP (BCRPR482). In 8226/Dox6 cells (Pgp), biricodar increases mitoxantrone and daunorubicin uptake by 55 and 100%, respectively, increases their retention by 100 and 60%, respectively, and increases their cytotoxicity 3.1- and 6.9-fold, respectively. Biricodar also increases the uptake, retention and cytotoxicity in HL60/Adr (MRP-1) and 8226/MR20 cells (BCRP(R482)), but has little effect in MCF7 AdVP3000 cells (BCRP(R482T))[1]. VX-710 is a non-macrocyclic pipecolinate derivative which binds the FK506 receptor protein. VX-710 has been shown to restore sensitivity in a range of multidrug-resistant cells, including myeloma, melanoma, carcinoma and leukaemia[2]. Biricodar effectively inhibits photoaffinity labeling of P-glycoprotein by [3H]azidopine or [125I]iodoaryl azido-prazosin with EC50 values of 0.75 and 0.55 μM[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.
Clinical Trial

分子量

603.71

Formula

C34H41N3O7
CAS 号

159997-94-1
中文名称

比立考达
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]. Minderman H, et al. VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Clin Cancer Res. 2004 Mar 1;10(5):1826-34.

    [2]. Yanagisawa T, et al. BIRICODAR (VX-710; Incel): an effective chemosensitizer in neuroblastoma. Br J Cancer. 1999 Jun;80(8):1190-6.

    [3]. Germann UA, et al. Cellular and biochemical characterization of VX-710 as a chemosensitizer: reversal of P-glycoprotein-mediated multidrug resistance in vitro. Anticancer Drugs. 1997 Feb;8(2):125-40.
Cell Assay
[1]

To study cytotoxicity in suspension cell lines, cells are plated in 96-well tissue culture plates at a density of 10,000 cells/well in RPMI 1640 supplemented with 10% FCS, 2 mM l-glutamine, 20 units/mL penicillin, and 20 μg/mL streptomycin. Drug is added to the culture medium to achieve final concentrations of 0.3 nM to 10 μM, with half-log increments, with and without biricodar at a final concentration of 2.5 μM. The final volume of medium per well is 100 μL. Cells are incubated for 96 h at 37°C in a fully humidified atmosphere of 5% CO2 in air. Cell growth is assessed by the WST-1 colorimetric assay[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]. Minderman H, et al. VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Clin Cancer Res. 2004 Mar 1;10(5):1826-34.

    [2]. Yanagisawa T, et al. BIRICODAR (VX-710; Incel): an effective chemosensitizer in neuroblastoma. Br J Cancer. 1999 Jun;80(8):1190-6.

    [3]. Germann UA, et al. Cellular and biochemical characterization of VX-710 as a chemosensitizer: reversal of P-glycoprotein-mediated multidrug resistance in vitro. Anticancer Drugs. 1997 Feb;8(2):125-40.

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

VX-11e

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。

VX-11e  纯度: 99.12%

VX-11e 是一种高效的，具有选择性的，可口服的 ERK 抑制剂，Ki 值 < 2 nM。

VX-11e

VX-11e Chemical Structure

CAS No. : 896720-20-0

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 ￥1046 In-stock
5 mg ￥950 In-stock
10 mg ￥1395 In-stock
50 mg ￥3720 In-stock
100 mg ￥6210 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VX-11e 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.

IC50 & Target

ERK2

2 nM (Ki)

GSK3

395 (Ki)

CDK2

852 (Ki)

AURA

540 (Ki)

体外研究
(In Vitro)

VX-11e is active in the HT29 cell proliferation assay (IC50=48 nM)[1].

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

VX-11e is orally bioavailable in both rat and mice[1]. VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth in NSG mice bearing human melanoma RPDX tumors. VX-11e with BKM120 significantly improves tumor growth inhibition[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

500.35

Formula

C24H20Cl2FN5O2
CAS 号

896720-20-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (199.86 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 1.9986 mL 9.9930 mL 19.9860 mL
5 mM 0.3997 mL 1.9986 mL 3.9972 mL
10 mM 0.1999 mL 0.9993 mL 1.9986 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: ≥ 3.25 mg/mL (6.50 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (6.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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

  • 2.

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

    Solubility: ≥ 3.25 mg/mL (6.50 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (6.50 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 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Aronov, Alex M., et al. Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control. Journal of Medicinal Chemistry (2009), 52(20), 6362-6368.

    [2]. Krepler C, et al. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies. Clin Cancer Res. 2016 Apr 1;22(7):1592-602.
Kinase Assay
[1]

Compounds are assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) is incubated with various concentrations of the compounds in DMSO (2.5%) for 10 min. at 30°C in 0.1 mol/L HEPES buffer, pH=7.5, containing 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase and 200 μM erktide peptide. The reaction is initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM is monitored.

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 Assay
[1]

Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter.

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]

Human melanoma RPDX tumors are expanded in vivo using NSG mice prior to the therapy experiments. Pooled tumor chunks banked from early mouse passages are implanted into 50 NSG mice (1:10 expansion). These tumors are harvested when reaching the maximum volume allowed on the protocol (1,000 mm3), digested, and banked as live cells. The larger part of this stock is retained as a master bank, and the other part is implanted at a 1:5 ratio into NSG mice to use in the therapy experiments. The expansion phase is under continuous drug pressure with PLX4720 200 ppm chemical additive diet at approximately clinical plasma levels. The plasma levels of PLX4720 (103.7 μg/mL ±3.2 after 7 days) are similar to steady-state levels in patients treated with vemurafenib 960 mg twice a day (130.6 μg/mL±71.78). When tumors have reached 200 mm3 per caliper measurement, animals are randomized into treatment groups followed by a 3-day ishout phase. Tumor size is assessed twice weekly per caliper measurement. Mice are sacrificed after two weeks of treatment or when necessary for animal welfare. Dosing is prolonged when tumor control is achieved as indicated. Tumor tissue is conserved in formalin (for FFPE) and snap-frozen in liquid N2 for protein extraction. Treatment groups are sacrificed 4 hours after last dose.

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]. Aronov, Alex M., et al. Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control. Journal of Medicinal Chemistry (2009), 52(20), 6362-6368.

    [2]. Krepler C, et al. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies. Clin Cancer Res. 2016 Apr 1;22(7):1592-602.

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

Amprenavir(Synonyms: 安瑞那韦; VX-478)

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。

Amprenavir (Synonyms: 安瑞那韦; VX-478) 纯度: 99.58%

Amprenavir (VX-478) 是HIV蛋白酶抑制剂，Ki为0.6 nM。Amprenavir 也是 SARS-CoV 3CLpro 的抑制剂，IC50 为 1.09 μM。

Amprenavir(Synonyms: 安瑞那韦; VX-478)

Amprenavir Chemical Structure

CAS No. : 161814-49-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥612 In-stock
5 mg ￥550 In-stock
25 mg ￥2500 In-stock
50 mg ￥3650 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Amprenavir 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Metabolism/Protease Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • CNS-Penetrant Compound Library
  • Peptidomimetic Library
  • Drug Repurposing Compound Library
  • Covalent Screening Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library

生物活性

Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.

IC50 & Target

IC50 Value: 0.6 nM (Ki); Against wild-type clinical HIV isolates:14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Target: HIV protease
体外研究
(In Vitro)

Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors. Amprenavir’s in vitro 50% inhibitory concentration (IC50) against wild-type clinical HIV isolates is 14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Amprenavir had direct inhibitory effects on invasion of Huh-7 hepatocarcinoma cell lines, inhibiting MMP proteolytic activation [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)

Amprenavir was able to promote regression of hepatocarcinoma growth in vivo by anti-angiogenetic and overall anti-tumor activities, independently by PI3K/AKT related pathways that at today is one of the more suggestive hypothesis to explain the anti-tumor effects of the different protease inhibitors [2]. Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increased plasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice [3]. Amprenavir has been approved for adults and children; the recommended capsule doses are 1200 mg twice daily for adults and 20 mg/kg twice daily or 15 mg/kg 3 times daily for children < 13 years of age or adolescents < 50 kg [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

505.63

Formula

C25H35N3O6S
CAS 号

161814-49-9
中文名称

安瑞那韦
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 (197.77 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 1.9777 mL 9.8887 mL 19.7773 mL
5 mM 0.3955 mL 1.9777 mL 3.9555 mL
10 mM 0.1978 mL 0.9889 mL 1.9777 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 (4.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.94 mM，饱和度未知) 的澄清溶液。

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

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

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.94 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

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

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

    Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.94 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]. Sadler BM, Stein DS. Clinical pharmacology and pharmacokinetics of amprenavir. Ann Pharmacother. 2002 Jan;36(1):102-18.

    [2]. Esposito V, Verdina A, Manente L, Amprenavir inhibits the migration in human hepatocarcinoma cell and the growth of xenografts. J Cell Physiol. 2013 Mar;228(3):640-5.

    [3]. Helsley RN, Sui Y, Ai N, Pregnane X Receptor Mediates Dyslipidemia Induced by the HIV Protease Inhibitor Amprenavir in Mice. Mol Pharmacol. 2013 Jun;83(6):1190-9.

    [4]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

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

Tezacaftor(Synonyms: VX-661)

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。

Tezacaftor (Synonyms: VX-661) 纯度: 99.92%

Tezacaftor (VX-661) 是 F508del CFTR 的矫正器，能够帮助 CFTR 蛋白与细胞表面结合。

Tezacaftor(Synonyms: VX-661)

Tezacaftor Chemical Structure

CAS No. : 1152311-62-0

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 ￥1260 In-stock
2 mg ￥700 In-stock
5 mg ￥1100 In-stock
10 mg ￥1500 In-stock
50 mg ￥4400 In-stock
100 mg ￥7200 In-stock
200 mg ￥12500 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Tezacaftor 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
  • Membrane Transporter/Ion Channel Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library

生物活性

Tezacaftor (VX-661) is a second F508del CFTR corrector and help CFTR protein reach the cell surface.

体外研究
(In Vitro)

In vitro, a combination of Tezacaftor (VX-661) and ivacaftor results in greater CFTR activity compared with Tezacaftor (VX-661) alone[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.
Clinical Trial

分子量

520.50

Formula

C26H27F3N2O6
CAS 号

1152311-62-0
运输条件

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

4°C, stored under nitrogen

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

DMSO : ≥ 100 mg/mL (192.12 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 1.9212 mL 9.6061 mL 19.2123 mL
5 mM 0.3842 mL 1.9212 mL 3.8425 mL
10 mM 0.1921 mL 0.9606 mL 1.9212 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 (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 (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。

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

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

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

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

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

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.80 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]. Treatment with VX-661 and Ivacaftor in a Phase 2 Study Resulted in Statistically Significant Improvements in Lung Function in People with Cystic Fibrosis Who Have Two Copies of the F508del Mutation. April 18, 2013

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

Tozasertib(Synonyms: VX 680; MK-0457)

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。

Tozasertib (Synonyms: VX 680; MK-0457) 纯度: 99.94%

Tozasertib (VX 680; MK-0457) 是 Aurora A/B/C 激酶抑制剂，Ki 值分别为 0.6，18，4.6 nM。

Tozasertib(Synonyms: VX 680; MK-0457)

Tozasertib Chemical Structure

CAS No. : 639089-54-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥891 In-stock
25 mg ￥810 In-stock
50 mg ￥1300 In-stock
100 mg ￥2100 In-stock
250 mg ￥3100 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Tozasertib 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • Cytoskeleton Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with Kis of 0.6, 18, 4.6 nM, respectively.

IC50 & Target

Aurora A

0.6 nM (Ki)

Aurora B

18 nM (Ki)

Aurora C

4.6 nM (Ki)

体外研究
(In Vitro)

Tozasertib induces similar cytotoxicity with IC50 of approximately 300 nM and exhibits an AUR B-like inhibitory phenotype of G2/M arrest, endoreduplication and apoptosis in BaF3 cells transfected with ABL or FLT-3 (mutant and wild type) kinases. Tozasertib prevents the CAL-62 proliferation in a time-dependent manner. Tozasertib treatment for 14 days significantly decreases the number and size of colonies by approximately 70% in the 8305C and 90% in the CAL-62, 8505C and BHT-101. Treatment of the different ATC cells with Tozasertib inhibits proliferation with the IC50 between 25 and 150 nM. The Tozasertib significantly impairs the ability of the different cell lines to form colonies in soft agar. Analysis of caspase-3 activity indicates that Tozasertib induces apoptosis in the different cell lines. CAL-62 cells exposed for 12 hours to Tozasertib show an accumulation of cells with ≥ 4N DNA content. Time-lapse analysis demonstrates that Tozasertib-treated CAL-62 cells exit metaphase without dividing. Moreover, histone H3 phosphorylation is abrogated following Tozasertib treatment[2]. Tozasertib has significant inhibitory activity against BCR-Abl bearing the T315I mutation in patient-derived samples[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.
Clinical Trial

分子量

464.59

Formula

C23H28N8OS
CAS 号

639089-54-6
中文名称

陶扎色替
运输条件

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

4°C, protect from light

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

DMSO : ≥ 106.67 mg/mL (229.60 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 2.1524 mL 10.7622 mL 21.5244 mL
5 mM 0.4305 mL 2.1524 mL 4.3049 mL
10 mM 0.2152 mL 1.0762 mL 2.1524 mL

*

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

In Vivo:

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

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

  • 1.

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

    Solubility: ≥ 2.08 mg/mL (4.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.48 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.48 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 (4.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.48 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]. Harrington EA, et al. VX-680, a potent and selective smallmolecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004; 10:262-7.

    [2]. Salah E, et al. Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.J Med Chem. 2011 Apr 14;54(7):2359-67. Epub 2011 Mar 18.

    [3]. Arlot-Bonnemains Y, et al. Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines. Endocr Relat Cancer. 2008 Jun;15(2):559-68
Kinase Assay
[3]

The consumption of ATP is coupled via the pyruvate kinase/lactic dehydrogenase enzyme pair to the oxidation of NADH, which can be monitored through the decrease in absorption at 340 nm. Reactions contains 100 mM Tris (pH 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM phosphoenolpyruvate, 0.6 mg/mL NADH, 75 units/mL pyruvate kinase, 105 units/mL lactate dehydrogenase, and 0.5 mM substrate peptide (sequence: EAIYAAPFAKKK). Reactions (75 μL) are started by adding sufficient kinase to bring the reactions to 30 nM kinase concentration and the decrease in absorbance is monitored over 30 minutes at 30°C in a microtiter plate spectrophotometer. Inhibitory constants are obtained through addition of 3.75 μL Tozasertib in 100% DMSO or DMSO alone. Ki values are calculated as follows, Ki=IC50/(1+[S]/Kd), where [S]=[ATP]=2.2 mM, and Kd (of ATP to Abl)=70 μM. These values are calculated assuming a Kd (ATP) of 70 μM for wild type and H396P Abl kinase domain.

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 Assay
[2]

The CAL-62 cells are cultured in the absence (dimethyl sulfoxide, DMSO) or the presence of 500  nM Tozasertib for different periods of time (1-5 days). The dose-dependent effects of Tozasertib on cell proliferation are evaluated by treating the different ATC cells for 4 days with different concentrations of the Aurora inhibitor (5-500 nM). The cells are pulse labeled with 30 mM BrdU for 2  hours before the end of the incubation time. The BrdU incorporation is analyzed by means of a colorimetric immunoassay using the cell proliferation ELISA kit. The results from Tozasertib-treated cells are compared with those observed in control cells and expressed as a fold of variation versus control.

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]

For the HL-60 study, female athymic NCr-nu mice are inoculated subcutaneously with 107 HL-60(TB) leukemia cells into the right axillary area. Treatment is administered i.p. b.i.d. after tumors reached 150−200 mm3. Tozasertib is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. Cisplatin, formulated in saline, is administered i.p. q.4.d. for a total of three injections, at a dose of 5.4 mg/kg. For the MIA PaCa-2 studies, female MF1 nude mice are inoculated with 107 MIA PaCa-2 cells into the dorsal flank. Treatment is administered i.p. b.i.d. after tumors reach 175 mm3. Tozasertib is prepared in a vehicle of 50% PEG 300 in 50 mM phosphate buffer. 5-fluorouracil, formulated in saline, is administered i.v. q.4.d. at a dose of 50 mg/kg. For the HCT116 study, female Hsd RH rnu/nu rats are inoculated with 107 HCT116 cells into the right flank. Treatment is administered once the tumors reached 700−950 mm3. Tozasertib is administered continuously through an indwelling femoral catheter, followed by a saline infusion for 4 d before repeating the dose cycle. For all studies, tumor volume is determined by caliper measurements three times a week.

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]. Harrington EA, et al. VX-680, a potent and selective smallmolecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med. 2004; 10:262-7.

    [2]. Salah E, et al. Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.J Med Chem. 2011 Apr 14;54(7):2359-67. Epub 2011 Mar 18.

    [3]. Arlot-Bonnemains Y, et al. Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines. Endocr Relat Cancer. 2008 Jun;15(2):559-68

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

美国Labnet VX-200漩涡混合器S0200-230V

发表于由

【简单介绍】

美国Labnet VX-200漩涡混合器S0200-230V可连续可调节速度使，适合于各种应用从温和的混合样品成悬浮状。有两种模式可供选择。接触模式（适合短时混合样品）和连续模式。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。大离心管，小离心管和酶标板等多种振荡板可供选择， 坚固的构造确保仪器的寿命期长，底座确保仪器不移动。

【详细说明】

美国Labnet VX-200漩涡混合器S0200-230V

产品描述：   

   美国Labnet VX-200漩涡混合器S0200-230V可连续可调节速度使，适合于各种应用从温和的混合样品成悬浮状。有两种模式可供选择。接触模式（适合短时混合样品）和连续模式。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。大离心管，小离心管和酶标板等多种振荡板可供选择， 坚固的构造确保仪器的寿命期长，底座确保仪器不移动。VX-200漩涡混合仪身体娇小适合各种场所，适合在4 到65℃范围。

技术特点

■ 两种模式：接触式或连续操作式

■大功率马达可对样品进行有效混合

■速度可连续任意变化控制

■试管、离心管及酶标板等多种振荡板可供选择  

■适合在冷藏室或培养箱内使用


技术参数：

技术参数


速度：

0~2850rpm

操作模式：

接触式或连续操作

操作温度：

室温以上4～65°C

尺寸(长X宽X高) ：

14X16X13cm

重量：

2.2kg

电压及频率：

230V,50Hz


订货信息


货号

详细信息

S0200-230V

VX-200漩涡混合器 标配CombiCup振荡板

S0200-21

24*1.5/2.0mL管，24*0.5mL和32*0.2mL管振荡板

S0200-22

一个微孔板或者64*0.2mL管或8*0.2mL八联管振荡板

S0200-23

8*15mL管或者8*12/13mm直径管振荡板

S0200-24

6*50mL管振荡板

S0200-25

12*1.5mL/2.0mL管振荡板，管水平放置

S0200-26

4*15mL管振荡板，管水平放置

S0200-27

5*50mL管振荡板，管水平放置

可选模块：

漩涡混合仪器VX-200/S0200-230V

发表于由

【简单介绍】

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

美国labnet经典款漩涡混合仪器VX-200/S0200-230V是漩涡混合仪中的经典!热卖不衰！两种模式：接触式或连续操作式。适合在冷藏室或培养箱内使用。

金畔生物科技，进口

【详细说明】

美国labnet经典款漩涡混合仪器VX-200/S0200-230V

名称：VX-200漩涡混合仪

品牌：美国Labnet

订货号：S0200-230V

    美国labnet漩涡混合仪VX-200，连续可调节速度，适合于各种应用从温和的混合样品成悬浮状。

  有两种模式可供选择。接触模式（适合短时混合样品）和连续模式。标配的CombiCup振荡板可以漩涡混合一个管也可以混合多根管。大离心管，小离心管和酶标板等多种振荡板可供选择， 坚固的构造确保仪器的寿命期长，底座确保仪器不移动。

  VX-200漩涡混合仪身体娇小适合各种场所，适合在4 到65℃范围。

美国labnet经典款漩涡混合仪器VX-200/S0200-230V

技术特点：

■  两种模式：接触式或连续操作式 

■  大功率马达可对样品进行有效混合 

■  速度可连续任意变化控制 

■  试管、离心管及酶标板等多种振荡板可供选择   

■  适合在冷藏室或培养箱内使用

速度： 

0~2850rpm

操作模式： 

接触式或连续操作

操作温度： 

室温以上4～65°C

尺寸（长X宽X高） ：

14X16X13cm

重量： 

2.2kg

电压及频率：

230V,50Hz

订货信息

货号

详细信息

S0200-230V

VX-200漩涡混合器标配CombiCup振荡板

S0200-21

24*1.5/2.0mL管，24*0.5mL和32*0.2mL管振荡板

S0200-22

一个微孔板或者64*0.2mL管或8*0.2mL八联管振荡板

S0200-23

8*15mL管或者8*12/13mm直径管振荡板

S0200-24

6*50mL管振荡板

S0200-25

12*1.5mL/2.0mL管振荡板，管水平放置

S0200-26

4*15mL管振荡板，管水平放置

S0200-27

5*50mL管振荡板，管水平放置

Gartisertib(Synonyms: VX-803; M4344; ATR inhibitor 2)

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。

Gartisertib (Synonyms: VX-803; M4344; ATR inhibitor 2) 纯度: 99.88%

Gartisertib (VX-803) 是一种 ATP 竞争性的，具有口服活性的，选择性的 ATR 抑制剂，Ki<150 pm。gartisertib 抑制 atr 驱动的磷酸化检查点激酶-1 (chk1) 磷酸化, ic50值为 8 nM。具有抗肿瘤活性。

Gartisertib(Synonyms: VX-803; M4344; ATR inhibitor 2)

Gartisertib Chemical Structure

CAS No. : 1613191-99-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5000 In-stock
5 mg ￥4200 In-stock
10 mg ￥7000 In-stock
50 mg ￥20000 In-stock
100 mg ￥30000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Gartisertib 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library

生物活性

Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pm. gartisertib potently inhibits atr-driven phosphorylated checkpoint kinase-1 (chk1) phosphorylation with an ic50 of 8 nM. Antitumor activity[1][2].

IC50 & Target[1]

ATR

<150 pM (Ki)

体内研究
(In Vivo)

In monotherapy efficacy studies Gartisertib shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression could be observed in triple-negative breast cancer xenograft models[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

541.55

Formula

C25H29F2N9O3
CAS 号

1613191-99-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (46.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8466 mL 9.2328 mL 18.4655 mL
5 mM 0.3693 mL 1.8466 mL 3.6931 mL
10 mM 0.1847 mL 0.9233 mL 1.8466 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.84 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
  • 2.

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

    Solubility: 2.08 mg/mL (3.84 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.84 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]. Frank T. Zenke, et al. Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Experimental and Molecular Therapeutics.

    [2]. Gorecki L, et al. Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy. Pharmacol Ther. 2020 Feb 26:107518.

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