1. Apoptosis
  2. MDM-2/p53
  3. PhiKan 083

PhiKan 083 

Cat. No.: HY-108637
Handling Instructions

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, and a relative binding affinity (Kd) of 150 μM in Ln229 cells.

For research use only. We do not sell to patients.

PhiKan 083 Chemical Structure

PhiKan 083 Chemical Structure

CAS No. : 880813-36-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 300 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Description

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], and a relative binding affinity (Kd) of 150 μM in Ln229 cells[3].

IC50 & Target

Kd: 167 μM (p53-Y220C)[1], 150 μM (p53Y220C, in Ln229 cells)[3]

In Vitro

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 doxorubicin (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W)[3].

Cell Viability Assay[1]

Cell Line: Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells
Concentration: 125 μM
Incubation Time: 48 hours
Result: Caused ∼70 ± 5% reduction in cell viability of variants of Ln229 cells.
Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 130 mg/mL (545.46 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1959 mL 20.9793 mL 41.9586 mL
5 mM 0.8392 mL 4.1959 mL 8.3917 mL
10 mM 0.4196 mL 2.0979 mL 4.1959 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (9.11 mM); Clear solution

  • 2.

    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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
Molecular Weight

238.33

Formula

C₁₆H₁₈N₂

CAS No.

880813-36-5

SMILES

CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PhiKan 083
Cat. No.:
HY-108637
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PhiKan 083

Cat. No.: HY-108637