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JB170

JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM) . JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase[1].

Product Specifications

CAS Number

[2705844-82-0]

UNSPSC

12352005

Target

Aurora Kinase; PROTACs

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/jb170.html

Purity

98.97

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC1=CC=CC(OC)=C1C2=NCC3=C(C4=C2C=C(C=C4)Cl)N=C(NC5=CC=C(C(OC)=C5)C(NCCOCCOCCNC(COC6=C7C(C(N(C7=O)C8CCC(NC8=O)=O)=O)=CC=C6)=O)=O)N=C3

Molecular Formula

C48H44ClFN8O11

Molecular Weight

963.36

References & Citations

[1]Adhikari B, et al. PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase. Nat Chem Biol. 2020;16 (11) :1179-1188.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Aurora A; Cereblon

Available Sizes

Curated Selection

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