1H-Isoindole-1,3(2H)-dione, 4-[[2-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]-2-oxoethyl]amino]-2-(2,6-dioxo-3-piperidinyl)- Chemical Properties

Density 

1.482±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 5.56 mg/mL (7.31 mM; ultrasonic and warming and heat to 60°C)

form 

Solid

pka

10.74±0.40(Predicted)

color 

White to yellow

1H-Isoindole-1,3(2H)-dione, 4-[[2-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]-2-oxoethyl]amino]-2-(2,6-dioxo-3-piperidinyl)- Usage And Synthesis

Uses

XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells[1].

Biological Activity

XY028-140 is a selective CDK4/CDK6 degrader. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells[1]. A375 melanoma and T47D breast cancer cells are treated with 0.3 or 1 μμ XY028-140 for 24 hours. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity[1]. T47D breast cancer cells are treated with 0.03, 0.1, 0.3, 1, or 3 μμ XY028-140 for 11 days. XY028-140 inhibits cancer cell proliferation in breast cancer cells[1].

IC 50

CDK4; CDK6; Cereblon

References

[1]. Jian Jin, et al. Compositions and methods for treating cdk4/6-mediated cancer. WO2018106870A1.

1H-Isoindole-1,3(2H)-dione, 4-[[2-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]-2-oxoethyl]amino]-2-(2,6-dioxo-3-piperidinyl)-(2229974-83-6)Related Product Information

• MS4078
• MS1943
• MS4077