Antitumor agent-81 |
| カタログ番号GC73363 |
Antitumor agent-81(化合物5a)は細胞毒性の低いp62-rnf168アゴニストであり、p62とrnf168の相互作用を増強する。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2765180-17-2
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');)
;)
Antitumor agent-81 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. Antitumor agent-81 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner.
Antitumor agent-81 (20 μM, 72 h) has an IC50 of 0.36 μM for the cancer cell line HCT116 and an IC50 of 1.18 μM for A549. It shows cytotoxicity against cancer cells A357, HeLa, HepG2, MCF-7, MDA-MB-231, MGC-803, and H2OS, but does not induce cell apoptosis and has lower toxicity towards normal cells MCF-10A[1].Antitumor agent-81 (1-5 μM; 24 h) affects the HR (homologous recombination)-mediated DSB repair in HCT-116 cells, contributing to its antitumor activity[1].Antitumor agent-81 enhances the interaction between P62 and RNF168 in HCT-116 cells, with a Kd of 20.97 μM[1].Antitumor agent-81 inhibits the catalytic activity of RNF168 and the E3 ligase activity of RNF168 in HCT-116 cells[1].
Antitumor agent-81 (12.5-100 mg/kg, i.p., single dose) has an MTD of 50 mg/kg in BALB/c mice, while in female nude mice, the MTD is 12.5 mg/kg[1].Antitumor agent-81 (5-10 mg/kg, i.p., single every 3 days for 22 days) promotes tumor apoptosis and inhibits tumor growth in mice[1].1.19Pharmacokinetic Parameters of Antitumor agent-81 in Female BALB/c nude mice[1].
References:
[1]. Wang FC, et al. A 1,2,3-Triazole Derivative of Quinazoline Exhibits Antitumor Activity by Tethering RNF168 to SQSTM1/P62. J Med Chem. 2022 Nov 4.
| Cas No. | 2765180-17-2 | SDF | |
| Formula | C19H19N7O3 | M.Wt | 393.4 |
| 溶解度 | DMSO : ≥ 60 mg/mL (152.52 mM) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5419 mL | 12.7097 mL | 25.4194 mL |
| 5 mM | 0.5084 mL | 2.5419 mL | 5.0839 mL |
| 10 mM | 0.2542 mL | 1.271 mL | 2.5419 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *