PhiKan 083
Based on 1 publication(s) in Google Scholar
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM. PhiKan 083 can be used for cancer research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.69%
- CAS. Nr.: 880813-36-5
- Formel: C16H18N2
- Molecular Weight:238.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) PhiKan 083
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Biologische Aktivität
Kd: 167 μM (p53-Y220C)[1], 150 μM (p53Y220C, in Ln229 cells)[3]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | IC50 |
43 μM
Compound: PK083; 1
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Antiproliferative activity against human BxPC3 cells harboring p53 Y220C mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human BxPC3 cells harboring p53 Y220C mutant after 72 hrs by CellTiter-Glo assay
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[PMID: 29702446] |
| NUGC-3 | IC50 |
14 μM
Compound: PK083; 1
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Antiproliferative activity against human NUGC3 cells harboring p53 Y220C mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human NUGC3 cells harboring p53 Y220C mutant after 72 hrs by CellTiter-Glo assay
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[PMID: 29702446] |
| NUGC-4 | IC50 |
9 μM
Compound: PK083; 1
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Antiproliferative activity against human NUGC4 cells harboring wild-type p53 after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human NUGC4 cells harboring wild-type p53 after 72 hrs by CellTiter-Glo assay
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[PMID: 29702446] |
| WI-38 | IC50 |
22 μM
Compound: PK083; 1
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Antiproliferative activity against human WI38 cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human WI38 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29702446] |
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells[3].
PhiKan 083 slows down its thermal denaturation rate[2].
PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells[3].
PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells
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Concentration:125 μM
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Incubation Time:48 hours
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Result:Caused ∼70 ± 5% reduction in cell viability of variants of Ln229 cells.
Chemical Information
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CAS. Nr. 880813-36-5
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Appearance Solid
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Molecular Weight 238.33
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Formel C16H18N2
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Color Light yellow to yellow
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SMILES
CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Impairing the interaction between Erg11 and cytochrome P450 reductase Ncp1 enhances azoles' antifungal activities. [Abstract]2025 Jul 24;16(1):6821. PMID: 40707518
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (419.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 100 mg/mL (419.59 mM; Need ultrasonic)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (9.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.17 mg/mL (9.11 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Boeckler FM, et al. Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10360-5. [Content Brief]
[2]. Rauf SM, et al. Effect of Y220C mutation on p53 and its rescue mechanism: a computer chemistry approach. Protein J. 2013 Jan;32(1):68-74. [Content Brief]
[3]. Paulmurugan R, et al. A protein folding molecular imaging biosensor monitors the effects of drugs that restore mutant p53 structure and its downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511. [Content Brief]
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. 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 / Ethanol | 1 mM | 4.1959 mL | 20.9793 mL | 41.9586 mL | 104.8966 mL |
| 5 mM | 0.8392 mL | 4.1959 mL | 8.3917 mL | 20.9793 mL | |
| 10 mM | 0.4196 mL | 2.0979 mL | 4.1959 mL | 10.4897 mL | |
| 15 mM | 0.2797 mL | 1.3986 mL | 2.7972 mL | 6.9931 mL | |
| 20 mM | 0.2098 mL | 1.0490 mL | 2.0979 mL | 5.2448 mL | |
| 25 mM | 0.1678 mL | 0.8392 mL | 1.6783 mL | 4.1959 mL | |
| 30 mM | 0.1399 mL | 0.6993 mL | 1.3986 mL | 3.4966 mL | |
| 40 mM | 0.1049 mL | 0.5245 mL | 1.0490 mL | 2.6224 mL | |
| 50 mM | 0.0839 mL | 0.4196 mL | 0.8392 mL | 2.0979 mL | |
| 60 mM | 0.0699 mL | 0.3497 mL | 0.6993 mL | 1.7483 mL | |
| 80 mM | 0.0524 mL | 0.2622 mL | 0.5245 mL | 1.3112 mL | |
| 100 mM | 0.0420 mL | 0.2098 mL | 0.4196 mL | 1.0490 mL |
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