XY028-140 (MS140)|CAS 2229974-83-6|DC Chemicals

Cas No.:	2229974-83-6
Chemical Name:	XY028-140
Synonyms:	XY028-140;MS140;s9880;4-((2-(4-(6-((6-acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido(2,3-d)pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)-2-oxoethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione;4-[[2-[4-[6-[(6-Acetyl-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]pi
SMILES:	O=C1C(C(C([H])([H])[H])=O)=C(C([H])([H])[H])C2=C([H])N=C(N([H])C3C([H])=C([H])C(=C([H])N=3)N3C([H])([H])C([H])([H])N(C(C([H])([H])N([H])C4=C([H])C([H])=C([H])C5C(N(C(C=54)=O)C4([H])C(N([H])C(C([H])([H])C4([H])[H])=O)=O)=O)=O)C([H])([H])C3([H])[H])N=C2N1C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
Formula:	C₃₉H₄₀N₁₀O₇
M.Wt:	760.7977
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	Distinct CDK6 complexes determine tumor cell response to CDK4/6 inhibitors and degraders-- Nature Cancer Pub Date : 2021-03-01 , DOI: 10.1038/s43018-021-00174-z

Description:

XY028-140 (MS140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).

Cat. No.	Product name	Field of application
DC67177	BTK-IN-29	BTK-IN-29 (compound 14) is an inhibitor of Btk.
DC65810	KT-333	KT-333 is a first-in-class molecular glue that induces selective degradation of STAT3 via the ubiquitin-proteasome system by simultaneously engaging STAT3 and the VHL E3 ligase. This novel mechanism enables potent STAT3 depletion with minimal off-target effects, demonstrating strong anti-tumor activity in hematologic malignancies.
DC55003	XY028-140 (MS140)	XY028-140 (MS-140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).
DC74522	WDR5 PROTAC MS40	MS40 is a cereblon (CRBN)-based proteolysis targeting chimera (PROTAC) degrader of the onco-target WD repeat domain 5 (WDR5) [1]. WDR5 is an integral component of the MLL/KMT2A lysine methyltransferase protein complex. The WDR5-binding component of MS40 is the selective inhibitor OICR-9429, and the CRBN-targeting moiety is the immunomodulatory drug pomalidomide. MS40 promotes degradation of WDR5 and the pomalidomide transcription factor neo-substrates IKZF1 and IKZF3.
DC12022	dBET6	dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.