TASIN-1
目录号 : GC11469
An inhibitor of truncated APC
Cas No.:792927-06-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
HCT116 (WT APC) and DLD1 (truncated APC1417) cell lines |
|
Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0.0001-100 μM; 48 h |
|
Applications |
TASIN-1 exhibited potent and selective toxicity toward DLD1 cells with IC50 value of 70 nM. TASIN-1 inhibited soft agar growth only in DLD1 cells. When cultured in medium with 0.1% serum for 7 days, HCT116 cells showed similar sensitivity to TASIN-1 as DLD1 cells. |
| Animal experiment [1]: | |
|
Animal models |
genetically engineered colorectal cancer (CRC) mouse model |
|
Dosage form |
20 mg/kg twice per week for 90 days or 40 mg/kg per week for 100 days (dissolved in 0.2 ml of solvent containing 10% DMSO and 10% cremophor); intraperitoneal injection |
|
Application |
In genetically engineered colorectal cancer (CRC) mouse model, TASIN-1 had a long retention time in mouse large intestinal tissue. TASIN-1 significantly reduced tumor formation in the colons. TASIN-1 did not induce obvious histological changes in livers, kidneys, or spleens of treated animals. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1] Lu Zhang, Panayotis C. Theodoropoulos, Ugur Eskiocak, et al. Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer. Science Translational Medicine 19 Oct 2016: Vol. 8, Issue 361, pp. 361ra140. | |
TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC) [1].
Adenomatous polyposis coli (APC) is a multifunctional tumor suppressor gene that is mutated in more than 80% of colon tumors. APC plays an important role in the negative regulation of canonical WNT signaling pathway through proteasomal degradation of b-catenin. APC is involved in cell cycle control, migration, differentiation, and apoptosis [1].
TASIN-1 is a selective inhibitor of mutant APC. In two authentic human CRC cell lines HCT116 (WT APC) and DLD1 (truncated APC1417), TASIN-1 exhibited potent and selective toxicity toward DLD1 cells with IC50 value of 70 nM but not toward HCT116 cells (IC50 >50 μM). TASIN-1 also reduced the endogenous cholesterol biosynthesis rate. TASIN-1 exerted its killing effects primarily by depleting cholesterol through inhibition of emopamil-binding protein (EBP) activity. However, knockdown of truncated APC (>90%) expression desensitized DLD1 cells to TASIN-1, suggesting that APC is required for TASIN-1's cytotoxicity [1].
In nude mice with established DLD1 and HT29 tumors, intraperitoneal injection of TASIN-1 twice daily for 18 days reduced the size of tumor xenografts and tumor growth rates. TASIN-1 resulted in the appearance of apoptotic cells with fragmented nuclei and induced an increase in cleaved caspase 3 and cleaved PARP1. However, TASIN-1 did not inhibit tumor growth in HCT116 (WT APC) xenografts. In a genetically engineered CRC mouse model, TASIN-1 significantly reduced tumor formation in the colons of CPC;Apc mice [1].
Reference:
1.Lu Zhang, Panayotis C. Theodoropoulos, Ugur Eskiocak, et al. Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer. Science Translational Medicine 19 Oct 2016: Vol. 8, Issue 361, pp. 361ra140.
| Cas No. | 792927-06-1 | SDF | |
| 化学名 | 1'-((4-methoxyphenyl)sulfonyl)-4-methyl-1,4'-bipiperidine | ||
| Canonical SMILES | CC1CCN(C2CCN(S(C3=CC=C(OC)C=C3)(=O)=O)CC2)CC1 | ||
| 分子式 | C18H28N2O3S | 分子量 | 352.49 |
| 溶解度 | ≥ 35.2mg/mL in DMSO | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.837 mL | 14.1848 mL | 28.3696 mL |
| 5 mM | 0.5674 mL | 2.837 mL | 5.6739 mL |
| 10 mM | 0.2837 mL | 1.4185 mL | 2.837 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。