2705844-82-0
Chemical Structure
JB170
- CAS No.: 2705844-82-0
- Formula:C48H44ClFN8O11
- Molecular Weight:963.36
IUPAC Name: 4-((9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido[4,5-e]azepin-2-yl)amino)-N-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)ethoxy)ethoxy)ethyl)-2-methoxybenzamide
InChIKey: GYKNPXCQINZRLL-UHFFFAOYSA-N
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
Biological Activity: 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].
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JB170 | 98.70% | 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. | ||||||||||||||||||||
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