Cat. No.: HY-187470

PROTAC AURKA degrader-4

PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC₅₀ of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia.
(Pink: Aurora A ligand (HY-168022); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-24057)).

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

CAS No.: 3135155-78-8
Formula: C₄₈H₄₈ClN₇O₈S
Molecular Weight:918.45

Storage:

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

PROTAC AURKA degrader-4 Chemical Structure

CAS No.: 3135155-78-8

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC₅₀ of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia^[1]. (Pink: Aurora A ligand (HY-168022); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-24057)).

IC₅₀ & Target

^[1]

Aurora A

Cereblon

All PROTACs Isoforms :

All Aurora Kinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	DC₅₀	25.62 nM	AURKA protein degradation in human Jurkat acute lymphoblastic leukemia cells assessed via Western blot after 6 h treatment. AURKA protein degradation in human Jurkat acute lymphoblastic leukemia cells assessed via Western blot after 6 h treatment.	42466758
Jurkat	IC50	0.81 μM	Antiproliferative activity against human Jurkat acute lymphoblastic leukemia cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human Jurkat acute lymphoblastic leukemia cells assessed as reduction in cell viability by CCK8 assay.	42466758
AGS	IC50	30.73 μM	Antiproliferative activity against human AGS gastric adenocarcinoma cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human AGS gastric adenocarcinoma cells assessed as reduction in cell viability by CCK8 assay.	42466758
IMR-32	IC50	2.12 μM	Antiproliferative activity against human IMR-32 neuroblastoma cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human IMR-32 neuroblastoma cells assessed as reduction in cell viability by CCK8 assay.	42466758
K562	IC50	24.19 μM	Antiproliferative activity against human K562 chronic myelogenous leukemia cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human K562 chronic myelogenous leukemia cells assessed as reduction in cell viability by CCK8 assay.	42466758
MOLT-4	IC50	4.46 μM	Antiproliferative activity against human Molt4 acute lymphoblastic leukemia cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human Molt4 acute lymphoblastic leukemia cells assessed as reduction in cell viability by CCK8 assay.	42466758
MV4-11	IC50	3.74 μM	Antiproliferative activity against human MV4-11 acute myeloid leukemia cells assessed as reduction in cell viability by CCK8 assay. Antiproliferative activity against human MV4-11 acute myeloid leukemia cells assessed as reduction in cell viability by CCK8 assay.	42466758
AGS	DC₅₀	>1000 nM	AURKA protein degradation in human AGS gastric adenocarcinoma cells assessed via Western blot after 6 h treatment. AURKA protein degradation in human AGS gastric adenocarcinoma cells assessed via Western blot after 6 h treatment.	42466758
IMR-32	DC₅₀	49.49 nM	AURKA protein degradation in human IMR-32 neuroblastoma cells assessed via Western blot after 6 h treatment. AURKA protein degradation in human IMR-32 neuroblastoma cells assessed via Western blot after 6 h treatment.	42466758
K562	DC₅₀	158.47 nM	AURKA protein degradation in human K562 chronic myelogenous leukemia cells assessed via Western blot after 6 h treatment. AURKA protein degradation in human K562 chronic myelogenous leukemia cells assessed via Western blot after 6 h treatment.	42466758
MOLT-4	DC₅₀	45.82 nM	AURKA protein degradation in human Molt4 acute lymphoblastic leukemia cells assessed via Western blot after 6 h treatment. AURKA protein degradation in human Molt4 acute lymphoblastic leukemia cells assessed via Western blot after 6 h treatment.	42466758
MV4-11	DC₅₀	30.39 nM	AURKA protein degradation in human MV4-11 acute myeloid leukemia cells assessed via Western blot after 6 h treatment. AURKA protein degradation in human MV4-11 acute myeloid leukemia cells assessed via Western blot after 6 h treatment.	42466758

In Vitro

PROTAC AURKA degrader-4 (12.7-1000 nM; 6 h) exhibits antiproliferative activity in various human cancer cell lines, with IC₅₀ values of 30.73 μM (AGS cells), 2.12 μM (IMR‑32 cells), 24.19 μM (K562 cells), 4.46 μM (Molt4 cells), 3.74 μM (MV4‑11 cells), and 0.81 μM (Jurkat cells)^[1].
PROTAC AURKA degrader-4 (0-10 μM; 24-48 h) induces dose-dependent G₂/M phase arrest and apoptosis in Jurkat cells, and upregulates the apoptotic markers cleaved caspase-3 and cleaved PARP^[1].
PROTAC AURKA degrader-4 (CT3) (12.7-1000 nM; 1-12 h) potently induces dose- and time-dependent degradation of AURKA in Jurkat cells, with a DC₅₀ of 25.62 nM and a maximum degradation rate of 88%^[1].
PROTAC AURKA degrader-4 (100 nM; 0-12 h) accelerates the degradation of AURKA protein in Jurkat cells, and when combined with Cycloheximide (HY-12320), it shortens the half-life of AURKA from 2.6 h to 0.4 h^[1].
PROTAC AURKA degrader-4 (100 nM; 2-6 h) mediates the degradation of AURKA in Jurkat cells via the ubiquitin-proteasome system, and its activity depends on simultaneous binding to both AURKA and CRBN^[1].
PROTAC AURKA degrader-4 (12.7-1000 nM; 2-6 h) disrupts the non-catalytic function of AURKA in Jurkat cells, attenuates its interactions with TPX2 and c-Myc, and downregulates c-MYC protein levels^[1].

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

Western Blot Analysis^[1]

Cell Line:

Jurkat cells
Concentration:

12.7, 37, 111, 333, 1000 nM (6 h); 100 nM (1-12 h); 300 nM (12 h)
Incubation Time:

1 h, 2 h, 4 h, 6 h, 8 h, 12 h
Result:

Reduced AURKA protein levels by 80.52% in Jurkat cells at 300 nM for 12 h.
Induced dose-dependent AURKA degradation across 12.7-1000 nM for 6 h, with a maximal degradation rate (Dmax) of 88% at 1000 nM and a DC₅₀ of 25.62 nM.
Triggered significant AURKA degradation as early as 1 h post-treatment at 100 nM, with maximal degradation observed at 8 h.

Cell Viability Assay^[1]

Cell Line:

AGS, IMR-32, K562, Molt4, MV4-11 cells
Concentration:

12.7, 37, 111, 333, 1000 nM
Incubation Time:

6 h
Result:

Had DC₅₀ values of >1000 nM (AGS), 49.49 nM (IMR-32), 158.47 nM (K562), 45.82 nM (Molt4), and 30.39 nM (MV4-11) for AURKA degradation, with robust degradation observed in IMR-32, Molt4, and MV4-11 cells.

Cell Cycle Analysis^[1]

Cell Line:

Jurkat cells
Concentration:

0, 0.3, 1, 3, 10 μM
Incubation Time:

48 h
Result:

Induced dose-dependent G2/M phase arrest in Jurkat cells.

Apoptosis Analysis^[1]

Cell Line:

Jurkat cells
Concentration:

0, 0.3, 1, 3, 10 μM
Incubation Time:

48 h
Result:

Induced dose-dependent apoptosis.

Western Blot Analysis^[1]

Cell Line:

Jurkat cells
Concentration:

0, 0.3, 1, 3, 10 μM
Incubation Time:

24, 48 h
Result:

Increased levels of Cyclin B1, cleaved caspase-3, and cleaved PARP in a dose-dependent manner via Western blot.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2
Rat^[1]	5 mg/kg	i.v.	110112 ng/mL	1.93 h

In Vivo

PROTAC AURKA degrader-4 (40 mg/kg; i.p.; once daily; for 16 consecutive days) achieves a tumor growth inhibition rate of 48.5% in Jurkat xenograft mice, while significantly degrading AURKA in tumor tissues and exhibiting favorable in vivo tolerance^[1].

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

Animal Model:

R-NSG nude mice (male, subcutaneous Jurkat cell xenograft model, tumors grown to ~150 mm³ before intervention)^[1]
Dosage:

40 mg/kg
Administration:

i.p.; once daily; 16 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 48.5%.
Significantly downregulated AURKA protein levels compared to vehicle and CAM2602-treated groups.
Caused no significant weight loss, indicating good tolerability.

Chemical Information

CAS No. 3135155-78-8
Molecular Weight 918.45
Formula C₄₈H₄₈ClN₇O₈S
SMILES

CC1=C(C=C(C2=C1NC=C2)C3=CC=C(C(OC4=NC=CC=C4)=C3)Cl)C(NS(=O)(N5CCN(CC5)C(CCCCCCCC#CC6=CC=C7C(CN(C7=O)C8CCC(NC8=O)=O)=C6)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ye Y, et al. Discovery of a Highly Subtype-Selective AURKA PROTAC Degrader (CT3) with Superior Activity to the Inhibitor for Hematological Malignancies. Journal of medicinal chemistry. 2026 Jul 17.

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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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PROTAC AURKA degrader-4

All PROTACs Isoforms

All Aurora Kinase Isoforms