CP 31398 dihydrochloride
目录号 : GC15840
A p53 stabilizing agent
Cas No.:1217195-61-3
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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CP 31398 dihydrochloride is a potent activator of p53 with maximum tolerated dose of 400 ppm [2].
Tumor protein p53 (p53) is a crucial protein in multicellular organisms and plays an important role in preventing cancer formation. Many studies have shown that activated p53 regulates the expression of p21 which binds to the G1-S/CDK complexes (molecules important for the G1/S transition in the cell cycle) and inhibits their activity [1].
CP 31398 dihydrochloride is a potent p53 stabilization and is regarded as a promising agent which combines with chemotherapy drugs for cancer treatment. When tested with a panel of 9 human cancer cell lines, CP 31398 dihydrochloride treatment resulted in cell apoptosis in mutant or wild-type p53 expressed cell lines (SW480, SKBr3, PA1, U20S, HCT116, and Saos-2) and enhanced chemotherapeutic drugs effect on cell killing while had no effect on cell lines not expressed p53 [1]. In four human HNSCC cell lines (JHU-O29, UMSCC-22A and Fadu), administration of CP 31398 dihydrochloride for 96 h inhibited the cell growth by accumulating p53 expression [2].
In colon adenocarcinomas F344 rast model, combination low dose of CP 31398 dihydrochloride with celecoxib markedly suppressed colon adenocarcinoma incidence (78%) and multiplicity (90%) by enhancing the expression of p53 which indicated that a combination of low dose CP-31398 dihydrochloride and celecoxib could be a promising therapy for colon cancer in clinic [3].
References:
[1]. Takimoto, R., et al., The mutant p53-conformation modifying drug, CP-31398, can induce apoptosis of human cancer cells and can stabilize wild-type p53 protein. Cancer Biol Ther, 2002. 1(1): p. 47-55.
[2]. Roh, J.L., et al., p53-Reactivating small molecules induce apoptosis and enhance chemotherapeutic cytotoxicity in head and neck squamous cell carcinoma. Oral Oncol, 2011. 47(1): p. 8-15.
[3]. Rao, C.V., et al., Inhibition of azoxymethane-induced colorectal cancer by CP-31398, a TP53 modulator, alone or in combination with low doses of celecoxib in male F344 rats. Cancer Res, 2009. 69(20): p. 8175-82.
| Cas No. | 1217195-61-3 | SDF | |
| 化学名 | (E)-N1-(2-(4-methoxystyryl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine dihydrochloride | ||
| Canonical SMILES | CN(C)CCCNC1=C2C=CC=CC2=NC(/C=C\C3=CC=C(OC)C=C3)=N1.Cl.Cl | ||
| 分子式 | C22H26N4O.HCl | 分子量 | 435.39 |
| 溶解度 | <43.54mg/ml in DMSO; <43.54mg/ml in Water | 储存条件 | 4°C, protect from light |
| 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 | 2.2968 mL | 11.484 mL | 22.9679 mL |
| 5 mM | 0.4594 mL | 2.2968 mL | 4.5936 mL |
| 10 mM | 0.2297 mL | 1.1484 mL | 2.2968 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。