BET-IN-12 

BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC₅₀ of 0.9 nM for BRD4^[1].

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

0.9 nM (BRD4)^[1]

BET-IN-12 (compound 15) (24 hours) displays BRD4 and c-Myc inhibition, MM proliferation with IC₅₀s values of 0.9 nM, 2.0 nM, and 6.0 nM, respectively^[1].
BET-IN-12 (compound 15) (24 hours) has high oxidative stability across species and low glucuronidation across species, so that translate into low orally administered minimum efficacious doses (MEDs) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BET-IN-12 (compound 15) is 100% oral bioavailability in mouse^[1].
BET-IN-12 (compound 15) impairs the growth of established PDX tumors (TGI = 88%) at MED = 2 mg/kg (AUC = 4800 nM•h)^[1].
pharmacokinetic (PK) profile^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

516.62

C₃₀H₂₉D₃FN₅O₂

1800343-11-6

CC(C)(O)C(C(F)=C1)=CC(N2[C@@H](C3CCOCC3)C4=CC=CC=C4)=C1C(N=C5)=C2C=C5C(N(N=N6)C)=C6C([2H])([2H])[2H]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hill, Matthew D., et al. Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties. ACS Med Chem Lett. 2022.