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Art. -Nr.: HY-179640

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SK4454

SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC₅₀ = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research.
(Pink: Aurora A ligand (HY-179643); Blue: Cereblon ligand (HY-179642); Black: linker (HY-69260)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₂H₅₀ClF₂N₁₁O₃
Molecular Weight:830.37

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

SK4454 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC₅₀ = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research^[1]. (Pink: Aurora A ligand (HY-179643); Blue: Cereblon ligand (HY-179642); Black: linker (HY-69260)).

IC₅₀ & Target^[1]

Aurora A

20 nM (IC₅₀)

Aurora A

1 nM (Ki)

Aurora B

7644 nM (Ki)

Cereblon

4060 nM ()

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

In Vitro

SK4454 (0.01-10000 nM, 1-48 h) induces degradation AURKA MYCN in neuroblastoma and benign cell lines HEK293T, RPE), exhibits the high potency in MYCN-amplified cells (IMR-32, NGP, SJNB-8; SK-N-BE(2)-C with DC₅₀s = 6 ,8 ,23 and 270 nM), shows reduced activity in other lines (SK-N-BE(2)-C, SK-N-AS, SJNB-1) with a hook effect, induces MYCN depletion as a secondary delayed consequence of AURKA degradation and requires concomitant engagement of both AURKA and CRBN to exert the degradation effect in MYCN amplified cells IMR-32, NGP, SJNB-8, SK-N-BE(2)-C with GI₅₀s = 8, 14, 53, 1111 nM;in non- amplified cells SK-N-SH, SK-N-AS and SJNB-1 with GI₅₀s = 430, 994, 13437nM;inbenign immortalized cell RPE with GI₅₀s = 221 nM^[1].
SK4454 (10-10000 nM, 72 h) effectively inhibits neuroblastoma cells (IMR-32, NGP, SJNB 8 , SKN-SH, SK-N-BE(2)-C and SJNB-1) growth^[1].
SK4454 (10-1000 nM, 24-72 h) is limited by MDR1-Mediated Drug Efflux in SKN-SH, SK-N-BE(2)-C, SJNB-1, NGP, SJNB-8, IMR-32B but SK-N-AS (due to the low CRBN expression)^[1].

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

Western Blot Analysis^[1]

Cell Line:

IMR-32
Concentration:

500 nM
Incubation Time:

1, 4, 24 and 48 h
Result:

Induced robust AURKA depletion already after 1 h, whereas MYCN co-depletion reached 50% only at 24h postexposure.

Cell Proliferation Assay^[1]

Cell Line:

IMR-32, NGP, SJNB 8 , SKN-SH, SK-N-BE(2)-C and SJNB-1
Concentration:

10, 100, 1000 and 10000 nM
Incubation Time:

72 h
Result:

Has The strongest antiproliferative effects with GI₅₀ values below 100 nM consistent with the observed potent AURKA degradation but less in SKN-SH, SK-N-BE(2)-C and SJNB-1.

Western Blot Analysis^[1]

Cell Line:

SK-N-BE(2)-C, SK-N-BE(2)-C, SK-N-SH, and SJNB-1
Concentration:

100 nM
Incubation Time:

24 h
Result:

Exhibit high expression of multidrug resistance protein 1 (MDR1), encoded by the ABCB1 gene in SK-N-BE(2)-C, SK-N-SH, and SJNB-1.
Exhibits the highest MDR1 expression in our panel, cotreatment with 1 μM Tariquidar (HY-10550) significantly enhanced the AURKA degradation.

Apoptosis Analysis^[1]

Cell Line:

NGP and SK-N-BE(2)-C cells
Concentration:

10, 100 and 1000 nM
Incubation Time:

48 h
Result:

Dose-dependently increased of caspase 3/7 activity.

Cell Proliferation Assay^[1]

Cell Line:

NGP, SJNB-8, and SK-N-BE(2)-C
Concentration:

10, 100 and 1000 nM
Incubation Time:

72 h
Result:

Exhibited growth-inhibitory activity comparable to AURKA inhibitor TAS-119, with nearly identical GI 50 values across cell lines.

Parmacokinetics

Species	Dose	Route	C_max	F	T_1/2	T_max	C₀	V_ss
Mice^[1]	15 mg/kg	i.p.	856 ng/mL	7 %	5.3 h	0.5 h	/	/
Mice^[1]	15 mg/kg	i.v.	/	/	3.4 h	/	11601 ng/mL	3.1 L/kg
Mice^[1]	30 mg/kg	p.o.	856 ng/mL	7 %	2.5 h	0.5 h	/	/

In Vivo

SK4454 (15 mg/kg, i.v. or i.p., once) induce AURKA protein depletion in IMR-32 neuroblastoma cell line-derived xenograft (CDX) mice^[1].

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

Animal Model:

IMR-32 cells (1 × 10 ⁷ cells in 0.2 mL volume) induced-female BALB/c nude mice^[1]
Dosage:

15 mg/kg
Administration:

i.v., or i.p. once
Result:

Reduced AURKA protein levels in vivo at 4 and 8 h post-treatment after a single IV dose, followed by a return to baseline levels at 24 h but not observed in i.p. group

Chemical Information

Molecular Weight 830.37
Formel C₄₂H₅₀ClF₂N₁₁O₃
SMILES

O=C(C1(CC2=NC(NC3=NNC(C)=C3)=CC=C2F)CCN(CC1)CC4=C(C(Cl)=CC=C4)F)N5CCC(CC5)CN6CCN(CC6)C7=CC=C(C=N7)N8C(NC(CC8)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Krols S, et al. Second-Generation AURKA-Targeting PROTACs: Structural Optimization toward in Vivo Degradation in Neuroblastoma. J Med Chem. 2025 Nov 27;68(22):23962-23976. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

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SK4454

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

SK4454 Related Classifications

HY-179640 Related Classifications