PhiKan 083 hydrochloride

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

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 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
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200 mg		Get quote

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Purity & Documentation
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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

Appearance

Solid

Formula

C₁₆H₁₉ClN₂

CAS No.

1050480-30-2

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)

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

*Please refer to the solubility information to select the appropriate solvent.

Purity & Documentation

Purity: 99.01%

Select Batch:

Data Sheet (278 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]