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Pyridostatin(Synonyms: RR82)

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Pyridostatin (Synonyms: RR82)

Pyridostatin (RR82) 是一种高选择性的 G-quadruplex DNA 稳定剂 (Kd=490 nM)。Pyridostatin 通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。Pyridostatin 靶向原癌基因 Src。Pyridostatin 降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。

Pyridostatin(Synonyms: RR82)

Pyridostatin Chemical Structure

CAS No. : 1085412-37-8

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Pyridostatin 的其他形式现货产品:

Pyridostatin hydrochloride

生物活性

Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2].

IC50 & Target

Kd: 490 nM (G-quadruplexe)[1]
体外研究
(In Vitro)

Pyridostatin (RR82) (10 μM; 48 hours) induces cell cycle arrest[1].
Pyridostatin is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin induces the formation of DNA DSBs. Remarkably, Pyridostatin (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[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.

Cell Viability Assay[1]

Cell Line: Over 60 different cancer cell lines
Concentration: 10 μM
Incubation Time: 48 hours
Result: Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.

分子量

596.64

Formula

C31H32N8O5
CAS 号

1085412-37-8
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]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.

    [2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.

    [3]. Moruno-Manchon JF, Koellhoffer EC, Gopakumar J, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.

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KB SRC 4

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KB SRC 4 

KB SRC 4 是一种有效的，高度选择性的 c-Src 抑制剂，Ki 和 Kd 值分别为 44 nM 和 86 nM，在浓度高达 125 μM 时，对 c-Abl 也无作用；KB SRC 4 具有抗肿瘤活性。

KB SRC 4

KB SRC 4 Chemical Structure

CAS No. : 1380088-03-8

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生物活性

KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.

IC50 & Target

Ki: 44 nM (c-Src)[1]
Kd: 86 nM (c-Src)[1]
体外研究
(In Vitro)

KB SRC 4 (Compound 4) is a potent, highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM. KB SRC 4 is selective between Src family members, with >2-fold selectivity over both Lck (Kd, 160 nM) and Fgr (Kd, 240 nM), 8-fold selectivity over c-Yes (Kd, 720 nM), and >40-fold selectivity over Lyn (Kd, 3200 nM), Hck (Kd, 4400 nM), and Fyn (Kd, >40000 nM). KB SRC 4 inhibits the growth of cancer cell lines, with GI50s of 11 μM, 12 μM, 11 μM, 6.0 μM against HT-29, SK-BR-3, MCF7, MDA-MB-453, and NIH-3T3, 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.
分子量

555.03

Formula

C32H23ClN8
CAS 号

1380088-03-8
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]. Brandvold KR, et al. Development of a highly selective c-Src kinase inhibitor. ACS Chem Biol. 2012 Aug 17;7(8):1393-8.

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英国Stuart SRC4小型强力循环冷却器

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【简单介绍】

英国Stuart SRC4小型强力循环冷却器（3L容量）是一种强力冷却器，设计紧凑，占用空间少，适合装在实验台上或台下。是一种强力冷却器，设计紧凑，占用空间少，适合装在实验台上或台下。LED 数字式显示器可清楚显示冷却介质的当前温度±2oC, 而设定温度只要一按按钮即可显示。
进口，质量保证！！

【详细说明】

英国Stuart SRC4小型强力循环冷却器（3L容量）

前言：

   安全功能再循环冷却器为外部设备提供了强大的冷却。通过精确控制的冷却介质的温度降低到-20℃，如冷凝操作的效率可以大大提高。循环冷却器是不是只比传统的水冷却的强大得多，但也是一个理想的替代品时，水的消耗是一个经济，环境和现实的原因的问题。SRC4提供了强大的冷却器，适合安装上或下一个紧凑的足迹一条长凳上。LED数码管显示清楚地表明当前冷却介质温度±2°C，而设定温度显示通过按下一个按钮。该单位的排水容易排空和清洗。它还集成了一个内置安全报警，表明制冷机组过载继电器。成立一个灰尘过滤器，可以不通过可拆卸的前面板的工具来访问。

特点：
数字设定温度
清楚地LED显示
运行安静
450W的冷却能力
自动安全切断功能

    英国Stuart小型强力循环冷却器SRC4（3L容量）给外部装置提供强力冷却。冷却介质的温度精确控制在-20oC，运行如冷凝的效率会大大提高。该再循环冷却器不但比传统的水冷却更有力，而且在经济、环保或现实原因水消耗成为问题时是一种理想的选择。

  英国Stuart小型强力循环冷却器SRC4（3L容量）是一种强力冷却器，设计紧凑，占用空间少，适合装在实验台上或台下。LED 数字式显示器可清楚显示冷却介质的当前温度±2oC, 而设定温度只要一按按钮即可显示。

本装置有专门排水管便于排空和清洁。 它也装有内置式安全报警装置，用于指示制冷装置的过载继电器。本装置还装有一个滤尘器， 通过拆下前仪表板，不用工具即可进入其中。

英国Stuart SRC4小型强力循环冷却器
技术参数

型号 SRC4
冷却能力 450W at 10?C
温度范围 -20 – +30?C
控制精度 ±2?C
冷却池容积 3 L
泵速 9 L /min
尺寸(w x d x h) 232 x 497 x 490mm
净重 25kg
电源 230V, 50Hz

订货信息

型号 描述
SRC4 循环冷却器，3 L容量
SRC14 循环冷却器，14 L容量

   

英国Stuart强力循环冷却器SRC4/SRC14（进口）

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【简单介绍】

英国Stuart强力循环冷却器SRC4/SRC14（进口）SRC4型是一种强力冷却器，设计紧凑，占用空间少，适合装在实验台上或台下。LED 数字式显示器可清楚显示冷却介质的当前温度±2oC, 而设定温度只要一按按钮即可显示。

进口，质量保证！！

【详细说明】

英国Stuart强力循环冷却器SRC4/SRC14（进口）

前言：

   安全功能再循环冷却器为外部设备提供了强大的冷却。通过精确控制的冷却介质的温度降低到-20℃，如冷凝操作的效率可以大大提高。循环冷却器是不是只比传统的水冷却的强大得多，但也是一个理想的替代品时，水的消耗是一个经济，环境和现实的原因的问题。SRC4提供了强大的冷却器，适合安装上或下一个紧凑的足迹一条长凳上。LED数码管显示清楚地表明当前冷却介质温度±2°C，而设定温度显示通过按下一个按钮。该单位的排水容易排空和清洗。它还集成了一个内置安全报警，表明制冷机组过载继电器。成立一个灰尘过滤器，可以不通过可拆卸的前面板的工具来访问。

特点：
数字设定温度
清楚地LED显示
运行安静
450W的冷却能力
自动安全切断功能

    英国Stuart强力循环冷却器SRC4/SRC14（进口）给外部装置提供强力冷却。冷却介质的温度精确控制在-20oC，运行如冷凝的效率会大大提高。该再循环冷却器不但比传统的水冷却更有力，而且在经济、环保或现实原因水消耗成为问题时是一种理想的选择。

SRC4型是一种强力冷却器，设计紧凑，占用空间少，适合装在实验台上或台下。LED 数字式显示器可清楚显示冷却介质的当前温度±2oC, 而设定温度只要一按按钮即可显示。

本装置有专门排水管便于排空和清洁。 它也装有内置式安全报警装置，用于指示制冷装置的过载继电器。本装置还装有一个滤尘器， 通过拆下前仪表板，不用工具即可进入其中。

SRC14具有SCR4的特点，它更适用于大容量场合，或者需要额外的冷却能力的条件下，如电子微处理器。该装置为地板立式，装有可锁定易转动自位轮，以保证其优异的可移动性。

技术参数

型号 SRC4 SRC14
冷却能力 450W at 10oC 1200W at 10oC
温度范围 -20 – +30oC -20 – +30oC
控制精度 ±2oC ±2oC
冷却池容积 3 L 14 L
泵速 9 L /min 18 L /min
尺寸(w x d x h) 232 x 497 x 490mm 354 x 384 x 851mm
净重 25kg 41kg
电源 230V, 50Hz 230V,50Hz

订货信息

型号 描述
SRC4 循环冷却器，3 L容量
SRC14 循环冷却器，14 L容量

  

T338C Src-IN-1

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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。

T338C Src-IN-1 

T338C Src-IN-1是突变型c-Src T338C高效抑制剂，IC50值111nM。对WT Src活性弱10倍以上。

T338C Src-IN-1

T338C Src-IN-1 Chemical Structure

CAS No. : 1351926-90-3

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生物活性

T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).

分子量

372.44

Formula

C17H20N6O2S
CAS 号

1351926-90-3
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]. Garske AL, et al. Chemical genetic strategy for targeting protein kinases based on covalent complementarity. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15046-52.

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T338C Src-IN-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。

T338C Src-IN-2 

T338C Src-IN-2是突变型c-Src激酶抑制剂，IC50值317nM，还能抑制T338C/V323A和T338C/V323S双突变Src活性，IC50值57和19nM。

T338C Src-IN-2

T338C Src-IN-2 Chemical Structure

CAS No. : 1351927-00-8

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生物活性

T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.

分子量

327.36

Formula

C17H18FN5O
CAS 号

1351927-00-8
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]. Garske AL, et al. Chemical genetic strategy for targeting protein kinases based on covalent complementarity. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15046-52.

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SU6656

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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。

SU6656  纯度: 96.87%

SU6656 是 Src 家族激酶抑制剂，抑制 Src，Yes，Lyn，Fyn 的 IC50分别为 280，20，130，170 nM。SU6656 可抑制 FAK Y576/577、 Y925、Y861 位点的磷酸化。SU6656 还能抑制p-AKT。

SU6656

SU6656 Chemical Structure

CAS No. : 330161-87-0

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 ￥869 In-stock
5 mg ￥790 In-stock
10 mg ￥1450 In-stock
50 mg ￥5100 In-stock
100 mg   询价  
200 mg   询价  

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SU6656 相关产品

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生物活性

SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.

体外研究
(In Vitro)

SU6656 decreases phosphorylation of Src family kinases (SFKs) in HNSCC 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.
体内研究
(In Vivo)

SU6656 (2-4 mg/kg; i.p.; once) significantly decreases ischemic postconditioning (IPoCo) mediated increase in fall down time[5].

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: Swiss albino male mice[5]
Dosage: 2, 4 mg/kg
Administration: Intraperitoneal injection; once
Result: Significantly decreased IPoCo mediated increase in fall down time.

分子量

371.45

Formula

C19H21N3O3S
CAS 号

330161-87-0
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 : 20 mg/mL (53.84 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6922 mL 13.4608 mL 26.9215 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL
10 mM 0.2692 mL 1.3461 mL 2.6922 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 mg/mL (5.38 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.38 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Blake RA, et al. SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling. Mol Cell Biol. 2000 Dec;20(23):9018-27.

    [2]. Veracini L, et al. Elevated Src family kinase activity stabilizes E-cadherin-based junctions and collective movement of head and neck squamous cell carcinomas. Oncotarget. 2014 Dec 26.

    [3]. Wu ML, et al. Divergent signaling pathways cooperatively regulate TGFβ induction of cysteine-rich protein 2 in vascular smooth muscle cells. Cell Commun Signal. 2014 Mar 28;12:22.

    [4]. Ondrusová L, et al. Inhibition of mTORC1 by SU6656, the selective Src kinase inhibitor, is not accompanied by activation of Akt/PKB signalling in melanoma cells. Folia Biol (Praha). 2013;59(4):162-7.

    [5]. Kumar A, et al. Pharmacological investigations on possible role of Src kinases in neuroprotective mechanism of ischemic postconditioning in mice. Int J Neurosci. 2014 Oct;124(10):777-86.

    [6]. Liu XF, et al. Antitumor effects of immunotoxins are enhanced by lowering HCK or treatment with SRC kinase inhibitors. Mol Cancer Ther. 2014 Jan;13(1):82-9.

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Src Inhibitor 3

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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。

Src Inhibitor 3  纯度: 98.61%

Src Inhibitor 3 是一种有效的、口服活性的 c 末端 Src 激酶 (CSK)，在 CSK HTRF 和 Caliper 实验中IC50 值分别为低于 3 nM 和 4 nM。Src Inhibitor 3 具有增强 T 细胞受体信号转导诱导的 T 细胞增殖的能力。

Src Inhibitor 3

Src Inhibitor 3 Chemical Structure

CAS No. : 2380027-49-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5910 In-stock
5 mg ￥4000 In-stock
10 mg ￥6800 In-stock
25 mg ￥13500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Src Inhibitor 3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library

生物活性

Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling[1].

IC50 & Target

IC50: <3 nm (c-terminal src kinase in csk htrf assay), 4 caliper assay)[1]
体内研究
(In Vivo)

Src Inhibitor 3 reduces inhibitory LCK phosphorylation in vivo upon oral dosing and shows the ability to enhance T cell activation in response to antigen stimulation[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

671.12

Formula

C34H32ClFN8O4
CAS 号

2380027-49-4
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 (149.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4900 mL 7.4502 mL 14.9005 mL
5 mM 0.2980 mL 1.4900 mL 2.9801 mL
10 mM 0.1490 mL 0.7450 mL 1.4900 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: ≥ 2.5 mg/mL (3.73 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.73 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。

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.10 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

*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]. O’Malley DP, et al. Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase. ACS Med Chem Lett. 2019 Sep 25;10(10):1486-1491.

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Src Inhibitor 1(Synonyms: Src Kinase Inhibitor 1; Src-l1)

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。

Src Inhibitor 1 (Synonyms: Src Kinase Inhibitor 1; Src-l1) 纯度: 99.98%

Src Inhibitor 1是高效选择性的，ATP-竞争性的双位点Src酪氨酸激酶抑制剂，对Src和Lck的IC50值分别为44 nM和88 nM。

Src Inhibitor 1(Synonyms: Src Kinase Inhibitor 1; Src-l1)

Src Inhibitor 1 Chemical Structure

CAS No. : 179248-59-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥575 In-stock
2 mg ￥500 In-stock
5 mg ￥700 In-stock
10 mg ￥950 In-stock
25 mg ￥2200 In-stock
50 mg ￥3950 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Src Inhibitor 1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library

生物活性

Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

IC50 & Target

IC50: 44 nM (Src), 88 nM (Lck)[1]
体外研究
(In Vitro)

Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[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

373.40

Formula

C22H19N3O3
CAS 号

179248-59-0
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 : 9.09 mg/mL (24.34 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6781 mL 13.3905 mL 26.7809 mL
5 mM 0.5356 mL 2.6781 mL 5.3562 mL
10 mM 0.2678 mL 1.3390 mL 2.6781 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: ≥ 0.91 mg/mL (2.44 mM); Clear solution

    此方案可获得 ≥ 0.91 mg/mL (2.44 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 9.1 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: ≥ 0.91 mg/mL (2.44 mM); Clear solution

    此方案可获得 ≥ 0.91 mg/mL (2.44 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 9.1 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]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.

    [2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
Kinase Assay
[2]

Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].

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

  • [1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.

    [2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

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多肽定制Biotin-RR-SRC, Insulin Receptor Tyrosine Kinase Substrate 编码

发表于由

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

名称 Biotin-RR-SRC, Insulin Receptor Tyrosine Kinase Substrate
编码
别名 Biotin-RR-SRC, Insulin Receptor Tyrosine Kinase Substrate
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） BIOTIN RRLIEDAEYAARG
序列（三字母缩写） Biotin -Arg-Arg-Leu-Ile-Glu-Asp-Ala-Glu-Tyr-Ala-Ala-Arg-Gly
基本描述
溶解度
分子量 1745.99
化学式 C74H120N24O23S
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Biotin-RR-SRC, Insulin Receptor Tyrosine Kinase Substrate 编码
Figures Biotin-RR-SRC, Insulin Receptor Tyrosine Kinase Substrate 编码
Reference
C端
N端
化学桥

MCB-613

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。

MCB-613  纯度: 99.95%

MCB-613 是一种有效的类固醇受体共激活因子 (SRC) 小分子“刺激物” (SMS)，超刺激 SRCs 的转录活性。 MCB-613 增加了 SRC 与其他共激活因子的相互作用，并显着诱导 ER 应激与活性氧 (ROS) 的产生相结合。 MCB-613 是一种 SMS，通过过度刺激 SRC 致癌程序，靶向癌基因用作抗癌药物。

MCB-613

MCB-613 Chemical Structure

CAS No. : 1162656-22-5

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 ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1900 In-stock
25 mg ￥3900 In-stock
50 mg ￥6200 In-stock
100 mg ￥9900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MCB-613 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Endoplasmic Reticulum Stress Compound Library

生物活性

MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program[1].

体外研究
(In Vitro)

MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells[1].
MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression[1].
MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO cells[1].

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

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 6 μM; 8 μM
Incubation Time: 24 hours
Result: Increased MMP13 mRNA expression.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 2 μM; 4 μM; 6 μM; 8 μM; 10 μM
Incubation Time: 24 hours
Result: Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression.

Cell Viability Assay[1]

Cell Line: SRC-3 KO and WT HeLa cells
Concentration: 3 μM; 4 μM; 5 μM; 6 μM; 7 μM
Incubation Time: 24 hours
Result: Decreased SRC-3 KO and WT HeLa cell viability.

体内研究
(In Vivo)

MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity[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: MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads)[1]
Dosage: 20 mg/kg
Administration: Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks
Result: Inhibited tumor growth in vivo.

分子量

304.39

Formula

C20H20N2O
CAS 号

1162656-22-5
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 : 50 mg/mL (164.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2853 mL 16.4263 mL 32.8526 mL
5 mM 0.6571 mL 3.2853 mL 6.5705 mL
10 mM 0.3285 mL 1.6426 mL 3.2853 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 (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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 (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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 (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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 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]. Wang L, et al. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52.

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

CGP77675

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。

CGP77675  纯度: 98.85%

CGP77675 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC50 分别为 20、150、1000、310 和 290 nM。具有抗肿瘤活性。

CGP77675

CGP77675 Chemical Structure

CAS No. : 234772-64-6

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥8250 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CGP77675 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
体外研究
(In Vitro)

CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells[1].

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

Cell Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx 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: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

分子量

443.54

Formula

C26H29N5O2
CAS 号

234772-64-6
运输条件

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

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献

  • [1]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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EPQpYEEIPIYL

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。

EPQpYEEIPIYL  纯度: 98.56%

EPQpYEEIPIYL 是一种磷酸肽，是 Src 同源 2 (SH2) 结构域配体。 EPQpYEEIPIYL 通过与 SH2 域结合来激活 Src 家族成员 (例如 Lck，Hck，Fyn)。

EPQpYEEIPIYL

EPQpYEEIPIYL Chemical Structure

CAS No. : 147612-86-0

规格 价格 是否有货 数量
1 mg ￥4000 In-stock
5 mg ￥14000 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

EPQpYEEIPIYL 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains[1][2].

体外研究
(In Vitro)

The hmT-derived phosphopeptide, pY324, which has the sequence EPQpYEEIPIYL, shows the highest affinity binding to GST fusion proteins of the Lck SH2 domain (5-fold higher than Lck’s affinity-for the Lck tail phosphopeptide) and the Src SH2 domain (44-fold higher than Src’s affinity for the Src tail phosphopeptide)[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

1473.52

Formula

C66H97N12O24P
CAS 号

147612-86-0
Sequence Shortening

EPQpYEEIPIYL
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 : 2 mg/mL (1.36 mM; ultrasonic and adjust pH to 2 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.6786 mL 3.3932 mL 6.7865 mL
5 mM — — —
10 mM — — —

*

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]. G Payne, et al. The phosphopeptide-binding specificity of Src family SH2 domains. Chem Biol. 1994 Oct;1(2):99-105.

    [2]. T D Mulhern, et al. The SH2 domain from the tyrosine kinase Fyn in complex with a phosphotyrosyl peptide reveals insights into domain stability and binding specificity. Structure. 1997 Oct 15;5(10):1313-23.

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多肽定制p60 v-src (137-157) 编码 [131023-24-0]

发表于由

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

名称 p60 v-src (137-157)
编码 [131023-24-0]
别名 p60 v-src (137-157)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） VAPSDSIQAEEWYFGKITRRE
序列（三字母缩写） Val-Ala-Pro-Ser-Asp-Ser-Ile-Gln-Ala-Glu-Glu-Trp-Tyr-Phe-Gly-Lys-Ile-Thr-Arg-Arg-Glu
基本描述
溶解度
分子量 2482.74
化学式 C111H168N30O35
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60 v-src (137-157) 编码 [131023-24-0]
Figures p60 v-src (137-157) 编码 [131023-24-0]
Reference
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N端
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多肽定制p60 v-src (137-157) 编码 [131023-24-0]

发表于由

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

名称 p60 v-src (137-157)
编码 [131023-24-0]
别名 p60 v-src (137-157)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） VAPSDSIQAEEWYFGKITRRE-OH
序列（三字母缩写） Val-Ala-Pro-Ser-Asp-Ser-Ile-Gln-Ala-Glu-Glu-Trp-Tyr-Phe-Gly-Lys-Ile-Thr-Arg-Arg-Glu
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60 v-src (137-157) 编码 [131023-24-0]
Figures p60 v-src (137-157) 编码 [131023-24-0]
Reference
C端
N端
化学桥

多肽定制p60c-src Substrate I 编码

发表于由

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

名称 p60c-src Substrate I
编码
别名 p60c-src Substrate I
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） YIYGSFK
序列（三字母缩写） H-Tyr-Ile-Tyr-Gly-Ser-Phe-Lys-OH (trifluoroacetate salt)
基本描述 Antigenic peptide presented by HLA-B44 that is recognized on human melanoma by autologous cytolytic Tlymphocytes.
溶解度
分子量 877.02
化学式 C44H60N8O11
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60c-src Substrate I 编码
Figures p60c-src Substrate I 编码
Reference
C端
N端
化学桥

多肽定制p60c-src Substrate II, Phosphorylated 编码

发表于由

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

名称 p60c-src Substrate II, Phosphorylated
编码
别名 p60c-src Substrate II, Phosphorylated
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） Ac-IY(PO3H2)GEF-NH2
序列（三字母缩写） Ac-Ile-Tyr(PO3H2)-Gly-Glu-Phe-NH2
基本描述
溶解度
分子量 748.8
化学式 C33H45N6O12P
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60c-src Substrate II, Phosphorylated 编码
Figures p60c-src Substrate II, Phosphorylated 编码
Reference
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N端
化学桥

多肽定制p60c-src Substrate I-Lys(Biotin) 编码 [198754-34-6]

发表于由

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

名称 p60c-src Substrate I-Lys(Biotin)
编码 [198754-34-6]
别名 p60c-src Substrate I-Lys(Biotin)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） YIYGSFK(BIOTIN)
序列（三字母缩写） Tyr-Ile-Tyr-Gly-Ser-Phe-Lys(Biotin)
基本描述
溶解度
分子量 1463.52
化学式 C62H94N16O25
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents p60c-src Substrate I-Lys(Biotin) 编码 [198754-34-6]
Figures p60c-src Substrate I-Lys(Biotin) 编码 [198754-34-6]
Reference
C端
N端
化学桥

CGP77675 hydrate

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。

CGP77675 hydrate 

CGP77675 hydrate 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 hydrate 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC50 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。

CGP77675 hydrate

CGP77675 hydrate Chemical Structure

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

* Please select Quantity before adding items.

CGP77675 hydrate 的其他形式现货产品:

CGP77675

生物活性

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
体外研究
(In Vitro)

CGP77675 hydrate dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 hydrate (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells[1].

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

Cell Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 hydrate (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[1].

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

Animal Model: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

Formula

C26H29N5O2.xH2O
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]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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

CGP77675 hydrate

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。

CGP77675 hydrate 

CGP77675 hydrate 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 hydrate 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC50 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC50 分别为 0.02、0.15、1.0、0.31 和 0.29 μM。具有抗肿瘤活性。

CGP77675 hydrate

CGP77675 hydrate Chemical Structure

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

* Please select Quantity before adding items.

CGP77675 hydrate 的其他形式现货产品:

CGP77675

生物活性

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].

IC50 & Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]
体外研究
(In Vitro)

CGP77675 hydrate dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1].
CGP77675 hydrate inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8 μM[1].
CGP77675 hydrate (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells[1].

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

Cell Viability Assay[1]

Cell Line: MC3T3-E1 cells
Concentration: 0.2, 1, and 5 μM
Incubation Time: 3 days
Result: Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis[1]

Cell Line: Src-overexpressing IC8.1 cells
Concentration: 0.04, 0.2, 1, 5, and 10 μM
Incubation Time: 2 hours
Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究
(In Vivo)

CGP77675 hydrate (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice[1].
CGP77675 hydrate (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[1].

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

Animal Model: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1]
Dosage: 1, 5, and 25 mg/kg
Administration: Injected s.c.; twice a day
Result: Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.
Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1]
Dosage: 10 and 50 mg/kg
Administration: Administered orally; twice a day for 6 weeks
Result: Partly prevented bone loss.

Formula

C26H29N5O2.xH2O
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]. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

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