ASR-490
目录号 : GC68701ASR-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。
Cas No.:2690312-67-3
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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 PARPExpression, 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. |
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].
| Animal Model: | Six- to 8-week-old BALB/c atmic nude mice (nu/nu) (pCMV/HCT116and 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. |
[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.
| Cas No. | 2690312-67-3 | SDF | Download SDF |
| 分子式 | C34H41NO7 | 分子量 | 575.69 |
| 溶解度 | DMSO : 25 mg/mL (43.43 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.737 mL | 8.6852 mL | 17.3705 mL |
| 5 mM | 0.3474 mL | 1.737 mL | 3.4741 mL |
| 10 mM | 0.1737 mL | 0.8685 mL | 1.737 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet