[CAS NO. 2990065-87-5] ADH-6TFA
PRODUCTS SPECIFICATIONS [2990065-87-5]
DESCRIPTION [2990065-87-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 754.67 |
| Molecular Formula | C31H37F3N8O11 |
| SMILES | O=C(C1=NC(OCCCN)=C(NC(C2=NC(OCCCN)=C(NC(C3=NC(OCCCC)=C([N+]([O-])=O)C=C3)=O)C=C2)=O)C=C1)OC.OC(C(F)(F)F)=O |
Summary
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] .
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
In Vivo
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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: | C max : 21 µg/mL, T 1/2 : 3.6 h |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 132.51 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.3251 mL | 6.6254 mL | 13.2508 mL |
| 5 mM | 0.2650 mL | 1.3251 mL | 2.6502 mL |
| 10 mM | 0.1325 mL | 0.6625 mL | 1.3251 mL |
