ADH-6 TFA |
カタログ番号GC65880
One-Click Copy Product Info
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ADH-6 TFA はトリピリジルアミド化合物です。 ADH-6 は、変異型 p53 DBD の凝集核形成サブドメインの自己組織化を無効にします。 ADH-6 TFA は、ヒト癌細胞の変異型 p53 凝集体を標的にして解離し、p53' の転写活性を回復させ、細胞周期の停止とアポトーシスを引き起こします。 ADH-6 TFA は、がん疾患の研究の可能性を秘めています。
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases[1].
ADH-6 (25 μM, 10 h) TFA inhibits aggregation of pR248W (indicated by dot blot assay)[1].
ADH-6 (5 μM, 6 h) TFA dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells[1].
ADH-6 (0-10 μM, 24 or 48 h) TFA causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2)[1].
ADH-6 (5 μM, 24 h) TFA specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells[1].
Cell Viability Assay[1]
| Cell Line: | MIA PaCa-2 (mutant R248W p53), SK-BR-3 (mutant R175H p53) |
| Concentration: | 0, 2.5, 5, 7.5, 10 μM |
| Incubation Time: | 24, 48 h |
| Result: | Caused death of cancer cells bearing mutant, but not WT, p53. |
Western Blot Analysis[1]
| Cell Line: | MIA PaCa-2 cells |
| Concentration: | 5 μM |
| Incubation Time: | 24 h |
| Result: | Increased expression of p53-inducible MDM2 and proapoptotic Bax. |
ADH-6 (intraperitoneal injection, 15 mg/kg, every 2 days, for a total of 12 doses) TFA causes regression of mutant p53-bearing tumors [1].
| Animal Model: | MIA PaCa-2 xenografts[1] |
| Dosage: | 716.4 µM in 0.02% DMSO |
| Administration: | Intraperitoneal injection, every 2 days, for a total of 12 doses |
| Result: | Reduced tumor growth relative to the saline-treated control group. Reduced mutant p53 levels and shrinked xenografts harboring aggregation-prone mutant p53. |
| Animal Model: | MIA PaCa-2 xenografts (pharmacokinetics assay)[1] |
| Dosage: | 15 mg/kg |
| Administration: | Intraperitoneal injection, for a single dose |
| Result: | Cmax: 21 µg/mL, T1/2: 3.6 h |
| Cas No. | SDF | ||
| Formula | C31H37F3N8O11 | M.Wt | 754.67 |
| 溶解度 | DMSO : 100 mg/mL (132.51 mM; Need ultrasonic) | Storage | Store at -20°C |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3251 mL | 6.6254 mL | 13.2508 mL |
| 5 mM | 265 μL | 1.3251 mL | 2.6502 mL |
| 10 mM | 132.5 μL | 662.5 μL | 1.3251 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 saline, 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)