N2'-((1r,4r)-4-aMinocyclohexyl)-5'-chloro-N6-(3-fluorobenzyl)-[2,4'-bipyridine]-2',6-diaMine-rel- Chemical Properties

Boiling point:

603.1±55.0 °C(Predicted)

Density 

1.302±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 50 mg/mL (117.39 mM; Need ultrasonic)

form 

Powder

pka

10.40±0.70(Predicted)

color 

Light yellow to yellow

N2'-((1r,4r)-4-aMinocyclohexyl)-5'-chloro-N6-(3-fluorobenzyl)-[2,4'-bipyridine]-2',6-diaMine-rel- Usage And Synthesis

Description

CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.

Uses

CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.

in vitro

In Vitro:CDK9-IN-2 (200 nM) reduces the expression of MEPCE indicating that MEPCE is a pharmacodynamic (PD) marker for any CDK9 inhibitor. The expression of MCL1 protein is reduced 2 hours after treatment and is further reduced after 16 hour exposure to CDK9-IN-2 (500 nM)[1].

IC 50

CDK9: 5 nM (IC₅₀, H929 multiple myeloma cell line)

References

References:[1]. Michel Faure, et al. Pharmacodynamic markers associated with cyclin-dependent kinase inhibitors. From PCT Int. Appl. (2012), WO 2012131594A1.