For research use only. Not for therapeutic Use.
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].
JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival[1].
JB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels [1].
JB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression[1].
JB170 (0.5 μM; 0-72 hours; MV4-11 cells) induces apoptosis is exclusively caused by targeting AURORA-A[1].
JB170 (0.1 μM; 0-9 hours; IMR5 cells) shows rapid AURORA-A depletion. JB170 (0~1 μM; 6 hours; MV4-11 cells) strongly attenuates in mutants with respect to AURORA-A. JB170 (0.1 μM; 18 hours; MV4-11 cells) does not activate AURORA-A. JB170 (0~1 μM; 24 hours; IMR5 cells) largely abrogates AURORA-AT217D depletion. JB170 (1 μM; 4 days; IMR5 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (IMR5 cells) reduces AURORA-A levels by lowering AURORA-A mRNA levels[1].
| Catalog Number | I045275 |
| CAS Number | 2705844-82-0 |
| Synonyms | 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-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]ethoxy]ethoxy]ethyl]-2-methoxybenzamide |
| Molecular Formula | C48H44ClFN8O11 |
| Purity | ≥95% |
| InChI | InChI=1S/C48H44ClFN8O11/c1-65-35-7-4-6-33(50)41(35)43-32-21-27(49)9-11-29(32)42-26(23-53-43)24-54-48(57-42)55-28-10-12-30(37(22-28)66-2)44(61)52-16-18-68-20-19-67-17-15-51-39(60)25-69-36-8-3-5-31-40(36)47(64)58(46(31)63)34-13-14-38(59)56-45(34)62/h3-12,21-22,24,34H,13-20,23,25H2,1-2H3,(H,51,60)(H,52,61)(H,54,55,57)(H,56,59,62) |
| InChIKey | GYKNPXCQINZRLL-UHFFFAOYSA-N |
| SMILES | COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)NCCOCCOCCNC(=O)COC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O)OC |
| Reference | [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. |
