PhiKan 083 hydrochloride

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

Cat. No.: HY-108637A Purity: 99.01%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

PhiKan 083 hydrochloride Chemical Structure

CAS No. : 1050480-30-2

Size	Price	Stock	Quantity
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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Based on 1 publication(s) in Google Scholar

Other Forms of PhiKan 083 hydrochloride:

PhiKan 083 In-stock

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Biological Activity
Purity & Documentation
References
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Description

PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a K_d of 167 μM^[1], and a relative binding affinity (K_d) of 150 μM in Ln229 cells^[3].

IC₅₀ & Target

Kd: 167 μM (p53-Y220C)^[1], 150 μM (p53^Y220C, 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 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

274.79

Formula

C₁₆H₁₉ClN₂

CAS No.

1050480-30-2

Appearance

Solid

Color

White to off-white

SMILES

CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (227.45 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (7.28 mM; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6391 mL	18.1957 mL	36.3914 mL
5 mM	0.7278 mL	3.6391 mL	7.2783 mL
10 mM	0.3639 mL	1.8196 mL	3.6391 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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

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Concentration _(final)

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In Vivo Dissolution Calculator

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Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.01%

Select Batch:

Data Sheet (277 KB) SDS (392 KB)

COA (253 KB) HNMR (251 KB) LCMS (93 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

H₂O / DMSO	1 mM	3.6391 mL	18.1957 mL	36.3914 mL	90.9786 mL
H₂O / DMSO	5 mM	0.7278 mL	3.6391 mL	7.2783 mL	18.1957 mL
DMSO	10 mM	0.3639 mL	1.8196 mL	3.6391 mL	9.0979 mL
	15 mM	0.2426 mL	1.2130 mL	2.4261 mL	6.0652 mL
	20 mM	0.1820 mL	0.9098 mL	1.8196 mL	4.5489 mL
	25 mM	0.1456 mL	0.7278 mL	1.4557 mL	3.6391 mL
	30 mM	0.1213 mL	0.6065 mL	1.2130 mL	3.0326 mL
	40 mM	0.0910 mL	0.4549 mL	0.9098 mL	2.2745 mL
	50 mM	0.0728 mL	0.3639 mL	0.7278 mL	1.8196 mL
	60 mM	0.0607 mL	0.3033 mL	0.6065 mL	1.5163 mL
	80 mM	0.0455 mL	0.2274 mL	0.4549 mL	1.1372 mL
	100 mM	0.0364 mL	0.1820 mL	0.3639 mL	0.9098 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.