ASR-490

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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。

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

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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.

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