标签归档：notch

Notch inhibitor 1

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。

Notch inhibitor 1  纯度: 99.81%

Notch inhibitor 1 是一种有效的 Notch 的抑制剂，对 Notch 1 和 Notch 3 的 IC50 值分别为 7.8 和 8.5 nM。可用于癌症的研究。

Notch inhibitor 1

Notch inhibitor 1 Chemical Structure

CAS No. : 1584647-27-7

规格 价格 是否有货 数量
5 mg ￥19500 In-stock
10 mg ￥34000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Notch inhibitor 1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer[1].

IC50 & Target

IC50: 7.8 nM (Notch 1), 8.5 nM (Notch 3)[1]
体外研究
(In Vitro)

Notch inhibitor 1 (Example 1) potently inhibits Notch signaling pathway[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

574.49

Formula

C26H25F7N4O3
CAS 号

1584647-27-7
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 : 13.12 mg/mL (22.84 mM; ultrasonic and warming and heat to 70°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7407 mL 8.7034 mL 17.4067 mL
5 mM 0.3481 mL 1.7407 mL 3.4813 mL
10 mM 0.1741 mL 0.8703 mL 1.7407 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: 1.31 mg/mL (2.28 mM); Clear solution; Need ultrasonic

    此方案可获得 1.31 mg/mL (2.28 mM) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 13.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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

  • 2.

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

    Solubility: 1.31 mg/mL (2.28 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.31 mg/mL (2.28 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 13.1 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
  • 3.

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

    Solubility: 1.31 mg/mL (2.28 mM); Clear solution; Need ultrasonic

    此方案可获得 1.31 mg/mL (2.28 mM) 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 13.1 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]. Ashvinikumar V. Gavai, et al. Bis(fluoroalkyl)-1,4-benzodiazepinone compounds as notch inhibitors. WO2014047372A1.

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

Notch 1 TFA

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。

Notch 1 TFA 

Notch 1 TFA (Notch homolog 1, translocation-associated) 可基因编码蛋白质 NOTCH 家族的成员。该 I 型跨膜蛋白家族成员具有共同的结构特征，包括由多个表皮生长因子样 (EGF) 重复序列组成的细胞外结构域和由多种不同结构域类型组成的细胞内结构域。

Notch 1 TFA

Notch 1 TFA 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.

生物活性

Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types[1].

体外研究
(In Vitro)

Notch 1 is shown to promote mouse luminal prostate cell survival and proliferation through the activation of the prosurvival NF-κB pathway[2].
Down-regulation of Notch 1 and Jagged1 in human prostate cancer cell lines decreases in vitro invasion and cell growth[2].

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

1614.81

Formula

C64H98N15F3O25S3
Sequence Shortening

NH2-CLDQIGEFQCICE-COOH
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]. NOTCH1 notch receptor 1 [Homo sapiens (human)] Gene ID: 4851, updated on 28-Oct-2019.

    [2]. Stoyanova T, et al. Activation of Notch1 synergizes with multiple pathways in promoting castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):E6457-E6466.

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

Notch 1 TFA

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。

Notch 1 TFA 

Notch 1 TFA (Notch homolog 1, translocation-associated) 可基因编码蛋白质 NOTCH 家族的成员。该 I 型跨膜蛋白家族成员具有共同的结构特征，包括由多个表皮生长因子样 (EGF) 重复序列组成的细胞外结构域和由多种不同结构域类型组成的细胞内结构域。

Notch 1 TFA

Notch 1 TFA 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.

生物活性

Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types[1].

体外研究
(In Vitro)

Notch 1 is shown to promote mouse luminal prostate cell survival and proliferation through the activation of the prosurvival NF-κB pathway[2].
Down-regulation of Notch 1 and Jagged1 in human prostate cancer cell lines decreases in vitro invasion and cell growth[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

1614.81

Formula

C64H98N15F3O25S3
Sequence Shortening

NH2-CLDQIGEFQCICE-COOH
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]. NOTCH1 notch receptor 1 [Homo sapiens (human)] Gene ID: 4851, updated on 28-Oct-2019.

    [2]. Stoyanova T, et al. Activation of Notch1 synergizes with multiple pathways in promoting castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):E6457-E6466.

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

Notch 1 TFA

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。

Notch 1 TFA 

Notch 1 TFA (Notch homolog 1, translocation-associated) 可基因编码蛋白质 NOTCH 家族的成员。该 I 型跨膜蛋白家族成员具有共同的结构特征，包括由多个表皮生长因子样 (EGF) 重复序列组成的细胞外结构域和由多种不同结构域类型组成的细胞内结构域。

Notch 1 TFA

Notch 1 TFA 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.

生物活性

Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types[1].

体外研究
(In Vitro)

Notch 1 is shown to promote mouse luminal prostate cell survival and proliferation through the activation of the prosurvival NF-κB pathway[2].
Down-regulation of Notch 1 and Jagged1 in human prostate cancer cell lines decreases in vitro invasion and cell growth[2].

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

1614.81

Formula

C64H98N15F3O25S3
Sequence Shortening

NH2-CLDQIGEFQCICE-COOH
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]. NOTCH1 notch receptor 1 [Homo sapiens (human)] Gene ID: 4851, updated on 28-Oct-2019.

    [2]. Stoyanova T, et al. Activation of Notch1 synergizes with multiple pathways in promoting castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):E6457-E6466.

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

ASR-490

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。

ASR-490 

ASR-490 通过下调 Notch1 信号传导降低 HCT116 和 SW620 细胞的活力。ASR-490 克服 Notch1 的过表达并抑制 HCT/Notch1 转染子的生长。ASR-490 在异种移植小鼠中抑制对照 (pCMV/HCT116) 和 Notch1/HCT116 的肿瘤生长。

ASR-490

ASR-490 Chemical Structure

CAS No. : 2690312-67-3

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

ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].

IC50 & Target

Notch1[1]
体外研究
(In Vitro)

ASR-490 (0-1.6 µM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells)[1]. ASR-490 (750 nM in HCT116 cells and 1.2 µM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells[1]. ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants[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: HCT116, SW620 cells
Concentration: 0-1.6 µM
Incubation Time: 24 h, 48 h
Result: Reduced the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells).

Apoptosis Analysis[1]

Cell Line: HCT116, SW620 cells
Concentration: 750 nM in HCT116 cells and 1.2 µM in SW620 cells
Incubation Time: 24 h
Result: Showed apoptotic cell death and upregulation the proapoptotic markers Bax and cleaved PARP Expression, inhibited the capability of colorectal cancer cells.

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 750 nM in 24 h, 600 nM in 48 h
Incubation Time: 24 h, 48 h
Result: Overcome Notch1 overexpression and inhibited the growth of HCT/Notch1 transfectants.

体内研究
(In Vivo)

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].

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

Animal Model: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts)[1].
Dosage: 5 mg/kg
Administration: i.p., thrice a week for 4 weeks
Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

分子量

575.69

Formula

C34H41NO7
CAS 号

2690312-67-3
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]. Tyagi A, et al. ASR490, a Small Molecule, Overrides Aberrant Expression of Notch1 in Colorectal Cancer. Mol Cancer Ther. 2020; 19(12):2422-2431.

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

ASR-490

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。

ASR-490 

ASR-490 通过下调 Notch1 信号传导降低 HCT116 和 SW620 细胞的活力。ASR-490 克服 Notch1 的过表达并抑制 HCT/Notch1 转染子的生长。ASR-490 在异种移植小鼠中抑制对照 (pCMV/HCT116) 和 Notch1/HCT116 的肿瘤生长。

ASR-490

ASR-490 Chemical Structure

CAS No. : 2690312-67-3

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

ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].

IC50 & Target

Notch1[1]
体外研究
(In Vitro)

ASR-490 (0-1.6 µM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells)[1]. ASR-490 (750 nM in HCT116 cells and 1.2 µM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells[1]. ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants[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: HCT116, SW620 cells
Concentration: 0-1.6 µM
Incubation Time: 24 h, 48 h
Result: Reduced the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells).

Apoptosis Analysis[1]

Cell Line: HCT116, SW620 cells
Concentration: 750 nM in HCT116 cells and 1.2 µM in SW620 cells
Incubation Time: 24 h
Result: Showed apoptotic cell death and upregulation the proapoptotic markers Bax and cleaved PARP Expression, inhibited the capability of colorectal cancer cells.

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 750 nM in 24 h, 600 nM in 48 h
Incubation Time: 24 h, 48 h
Result: Overcome Notch1 overexpression and inhibited the growth of HCT/Notch1 transfectants.

体内研究
(In Vivo)

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].

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

Animal Model: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts)[1].
Dosage: 5 mg/kg
Administration: i.p., thrice a week for 4 weeks
Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

分子量

575.69

Formula

C34H41NO7
CAS 号

2690312-67-3
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]. Tyagi A, et al. ASR490, a Small Molecule, Overrides Aberrant Expression of Notch1 in Colorectal Cancer. Mol Cancer Ther. 2020; 19(12):2422-2431.

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

ASR-490

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。

ASR-490 

ASR-490 通过下调 Notch1 信号传导降低 HCT116 和 SW620 细胞的活力。ASR-490 克服 Notch1 的过表达并抑制 HCT/Notch1 转染子的生长。ASR-490 在异种移植小鼠中抑制对照 (pCMV/HCT116) 和 Notch1/HCT116 的肿瘤生长。

ASR-490

ASR-490 Chemical Structure

CAS No. : 2690312-67-3

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

ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[1].

IC50 & Target

Notch1[1]
体外研究
(In Vitro)

ASR-490 (0-1.6 µM; 24 h, 48 h) reduces the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells)[1]. ASR-490 (750 nM in HCT116 cells and 1.2 µM in SW620 cells, 24 h) shows apoptotic cell death and upregulation of the proapoptotic markers Bax and cleaved PARP Expression; inhibits the capability of colorectal cancer cells[1]. ASR-490 (HCT116 cells; 750 nM in 24 h, 600 nM in 48 h) overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants[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: HCT116, SW620 cells
Concentration: 0-1.6 µM
Incubation Time: 24 h, 48 h
Result: Reduced the viability of HCT116 and SW620 cells in 24h (IC50 =750 nM in HCT116 cells, IC50 =1.2 µM in SW620 cells) and 48h (IC50 =600 nM in HCT116 cells, IC50 =850 nM in SW620 cells).

Apoptosis Analysis[1]

Cell Line: HCT116, SW620 cells
Concentration: 750 nM in HCT116 cells and 1.2 µM in SW620 cells
Incubation Time: 24 h
Result: Showed apoptotic cell death and upregulation the proapoptotic markers Bax and cleaved PARP Expression, inhibited the capability of colorectal cancer cells.

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 750 nM in 24 h, 600 nM in 48 h
Incubation Time: 24 h, 48 h
Result: Overcome Notch1 overexpression and inhibited the growth of HCT/Notch1 transfectants.

体内研究
(In Vivo)

ASR-490 (5 mg/kg; i.p.; thrice a week for 4 weeks) inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice[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: Six- to 8-week-old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts)[1].
Dosage: 5 mg/kg
Administration: i.p., thrice a week for 4 weeks
Result: Inhibited the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice.

分子量

575.69

Formula

C34H41NO7
CAS 号

2690312-67-3
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]. Tyagi A, et al. ASR490, a Small Molecule, Overrides Aberrant Expression of Notch1 in Colorectal Cancer. Mol Cancer Ther. 2020; 19(12):2422-2431.

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IMR-1

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。

IMR-1  纯度: 98.88%

IMR-1 是一种 Notch 抑制剂， IC50 为 26 μM。IMR-1 阻止 Maml1 募集到染色质上的 Notch 三元复合体 (NTC)，抑制 Notch 靶基因转录，既有抗肿瘤活性。

IMR-1

IMR-1 Chemical Structure

CAS No. : 310456-65-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1050 In-stock
5 mg ￥550 In-stock
10 mg ￥950 In-stock
50 mg ￥3800 In-stock
100 mg ￥6300 In-stock
200 mg   询价  
500 mg   询价  

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IMR-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Neuronal Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Transcription Factor Targeted Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth[1].

IC50 & Target

IC50: 26 nM (Notch)[1]
体内研究
(In Vivo)

IMR-1 (i.p.; 15mg/kg; for 28 days) inhibits Notch-dependent tumor growth in patient-derived 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.

Animal Model: Nude mouses with adenocarcinoma xenograft[1]
Dosage: 15mg/kg
Administration: I.p.; for 28 days
Result: Blocks tumor establishment.

分子量

353.41

Formula

C15H15NO5S2
CAS 号

310456-65-6
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 (282.96 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 2.8296 mL 14.1479 mL 28.2957 mL
5 mM 0.5659 mL 2.8296 mL 5.6591 mL
10 mM 0.2830 mL 1.4148 mL 2.8296 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 (7.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.07 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 (7.07 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.07 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 (7.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.07 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]. Astudillo L et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603.

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