PhiKan 083

Name: PhiKan 083
Brand: MedChemExpress
SKU: HY-108637
Rating: 4.5 (1 reviews)

Cat. No.: HY-108637 Purity: 98.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a K_d of 167 μM. PhiKan 083 can be used for cancer research.

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

PhiKan 083 Chemical Structure

CAS No. : 880813-36-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	In-stock	Estimated Time of Arrival: December 31
Solid
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	USD 420	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PhiKan 083:

PhiKan 083 hydrochloride In-stock

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References
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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 K_d of 167 μM. PhiKan 083 can be used for cancer research^[1].

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	43 μM Compound: PK083; 1	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	[PMID: 29702446]
NUGC-3	IC₅₀	14 μM Compound: PK083; 1	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	[PMID: 29702446]
NUGC-4	IC₅₀	9 μM Compound: PK083; 1	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	[PMID: 29702446]
WI-38	IC₅₀	22 μM Compound: PK083; 1	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	[PMID: 29702446]

In Vitro

PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a K_d of 167 μM^[1], shows a relative binding affinity (K_d) of 150 μM for p53^Y220C 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 (p53^wt, p53^Y220C, p53^G245S, p53^R282W)^[3].

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

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.

Molecular Weight

238.33

Formula

C₁₆H₁₈N₂

CAS No.

880813-36-5

Appearance

Solid

Color

Colorless to light yellow

SMILES

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

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

In Vitro:

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)

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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.49 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

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.
Protocol 3

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.93%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (251 KB) RP-HPLC (87 KB)

Handling Instructions (2659 KB)

References

[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

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

PhiKan 083 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PhiKan 083880813-36-5PhiKan083PhiKan-083MDM-2/p53Inhibitorinhibitorinhibit

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PhiKan 083

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Complete Stock Solution Preparation Table

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