XY028-140

• CAT Number: I044696
• CAS Number: 2229974-83-6
• Molecular Formula: C39H40N10O7
• Molecular Weight: 760.80
• Purity: ≥95%
• Synonyms: 4-[[2-[4-[6-[(6-acetyl-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]piperazin-1-yl]-2-oxoethyl]amino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
• InChI: InChI=1S/C39H40N10O7/c1-21-26-19-42-39(45-34(26)48(23-6-3-4-7-23)37(55)32(21)22(2)50)43-29-12-10-24(18-41-29)46-14-16-47(17-15-46)31(52)20-40-27-9-5-8-25-33(27)38(56)49(36(25)54)28-11-13-30(51)44-35(28)53/h5,8-10,12,18-19,23,28,40H,3-4,6-7,11,13-17,20H2,1-2H3,(H,44,51,53)(H,41,42,43,45)
• InChIKey: IWFNIKIERKCKFZ-UHFFFAOYSA-N
• SMILES: CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCN(CC4)C(=O)CNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8CCCC8)C(=O)C

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].
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].

Reference

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

[2]. Xuewei Wu, et al. Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders. Nat Cancer 2, 429-443 (2021).