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> ADH-6 (TFA) [2990065-87-5]

ADH-6 (TFA) [2990065-87-5]

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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.

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ADH-6 TFA Chemical Structure

ADH-6 TFA Chemical Structure

CAS No. : 2990065-87-5

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of ADH-6 TFA:

  • ADH-6 Obtenir un devis
Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ADH-6 TFA Related Antibodies

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].

MedChemExpress (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: Cmax: 21 µg/mL, T1/2: 3.6 h
Masse moléculaire

754.67

Formule

C31H37F3N8O11
CAS No.

2990065-87-5
Appearance

Solid

Color

Off-white to light yellow

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (132.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Pureté et documentation

Purity: 99.91%

COA (252 KB) HNMR (121 KB) RP-HPLC (223 KB) MS (162 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Palanikumar L, et al. Protein mimetic amyloid inhibitor potently abrogates cancer-associated mutant p53 aggregation and restores tumor suppressor function. Nat Commun. 2021;12(1):3962.  [Content Brief]

  • [1]. Palanikumar L, et al. Protein mimetic amyloid inhibitor potently abrogates cancer-associated mutant p53 aggregation and restores tumor suppressor function. Nat Commun. 2021;12(1):3962.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3251 mL 6.6254 mL 13.2508 mL 33.1271 mL
5 mM 0.2650 mL 1.3251 mL 2.6502 mL 6.6254 mL
10 mM 0.1325 mL 0.6625 mL 1.3251 mL 3.3127 mL
15 mM 0.0883 mL 0.4417 mL 0.8834 mL 2.2085 mL
20 mM 0.0663 mL 0.3313 mL 0.6625 mL 1.6564 mL
25 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3251 mL
30 mM 0.0442 mL 0.2208 mL 0.4417 mL 1.1042 mL
40 mM 0.0331 mL 0.1656 mL 0.3313 mL 0.8282 mL
50 mM 0.0265 mL 0.1325 mL 0.2650 mL 0.6625 mL
60 mM 0.0221 mL 0.1104 mL 0.2208 mL 0.5521 mL
80 mM 0.0166 mL 0.0828 mL 0.1656 mL 0.4141 mL
100 mM 0.0133 mL 0.0663 mL 0.1325 mL 0.3313 mL
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ADH-6 TFA Related Classifications

  • Apoptosis
  • MDM-2/p53 Apoptosis
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Keywords:

ADH-62990065-87-5ADH6ADH 6MDM-2/p53ApoptosisTripyridylamideself-assemblyp53transcriptionalcell cycleapoptosiscancerInhibitorinhibitorinhibit