JB170

JB170 is a potent and highly specific PROTAC-mediated AURORA-A 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.

Product information

Molecular Weight: 963.36

Formula: C48H44ClFN8O11

Chemical 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

Smiles: COC1C=C(C=CC=1C(=O)NCCOCCOCCNC(=O)COC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O)NC1=NC=C2CN=C(C3=C(F)C=CC=C3OC)C3=CC(Cl)=CC=C3C2=N1

InChiKey: GYKNPXCQINZRLL-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JB170 (1 μM; 24-72 hours; MV4-11 cells) mediates Aurora-A depletion inhibiting cancer cell survival. JB170 (0.01-10 μM; 6 hours; MV4-11 cells) reduces AURORA-A levels . JB170 (0.5 μM; 12 hours; MV4-11 cells) delays/arrests S-phase progression. JB170 (0.5 μM; 0-72 hours; MV4-11 cells) induced apoptosis is exclusively caused by targeting AURORA-A. 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.

Products are for research use only. Not for human use.