| Identification | Back Directory | [Name]
Benzamide, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-N-[2-[2-[2-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]ethoxy]ethoxy]ethyl]-2-methoxy- | [CAS]
2705844-82-0 | [Synonyms]
JB170
Benzamide, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-N-[2-[2-[2-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]ethoxy]ethoxy]ethyl]-2-methoxy- | [Molecular Formula]
C48H44ClFN8O11 | [MOL File]
2705844-82-0.mol | [Molecular Weight]
963.36 |
| Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear (Warmed) | [form ]
Solid | [pka]
10.68±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
JB170 is a highly specific AURORA-A degrader (PROTAC) comprising aurora kinase inhibitor alisertib connected to the CEREBLON-binding molecule thalidomide. JB170 induces rapid and durable degradation of AURORA-A in cancer cells leading to strong S-phase arrest and apoptosis. | [IC 50]
Aurora A: 28 nM (DC50); Aurora A: 99 nM (Kd); Aurora A: 193 nM (EC50); Cereblon | [References]
[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. DOI:10.1038/s41589-020-00652-y |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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