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).

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
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DC67513	MS8847	MS8847 represents a novel PROTAC molecule that selectively targets EZH2 for degradation by recruiting the VHL E3 ubiquitin ligase complex. This compound mediates potent, proteasome-dependent elimination of EZH2, demonstrating significant anti-proliferative effects against both AML and TNBC cell lines.
DC67512	PROTAC BRD4 Degrader-21	PROTAC BRD4 Degrader-21 (Compound 74) is a potent and selective degrader of BRD4, demonstrating robust tumor growth suppression in mouse xenograft models. Its efficacy supports its potential as a promising candidate for anticancer drug development.
DC67462	YJ1206	YJ1206 is an orally bioavailable PROTAC compound that selectively degrades CDK12 and CDK13, demonstrating potent activity (IC50 = 12.55 nM) in VCaP cells. It induces DNA damage, triggers apoptosis, and drives tumor regression in treatment-resistant prostate cancer PDX models, highlighting its therapeutic potential.
DC60681	SD-436	SD-436 is a highly potent and selective STAT3 degrader with DC50 of 0.1 nM in human PBMCs and displays >10,000-fold degradation selectivity for STAT3 over other STAT proteins.
DC65811	KT-253	KT-253 is a potent small molecule that stabilizes p53 while simultaneously acting as a PROTAC to degrade MDM2 (DC50 = 0.4 nM). It demonstrates strong antiproliferative effects in RS4;11 leukemia cells (IC50 = 0.3 nM), inducing G2/M cell cycle arrest and apoptosis. In vivo studies confirm its antitumor activity in mouse models.
DC60510	Iso-A11B5C1	Iso-A11B5C1 is an ionizable lipid. The iso-A11B5C1 LNP demonstrates a high level of muscle-specific mRNA delivery efficiency. exhibiting transfection efficiency comparable to the commercially available lipid SM-102, while considerably reducing inadvertent mRNA expression in main organs such as the liver and spleen.Additionally, study results show that intramuscular administration of mRNA formulated with iso-A11B5C1 LNP caused potent cellular immune responses, even with limited expression observed in lymph nodes.
DC65324	NX-2127	NX-2127 is a potent, selective, and orally bioavailable BTK degrader with Kd of 18 nM (for WT BTK), 45 nM (BTK C481S), 18 nM (BTK T474I), 44 nM (BTK M437R), 97 nM (BTK V416L), and 88 nM (BTK L528W), respectively. NX-2127 efficiently engages the intracellular ubiquitin-proteasome system to simultaneously bind both BTK and the CRBN E3 ubiquitin ligase complex, inducing polyubiquitination and proteasome-dependent degradation of BTK, IKZF1, and IKZF3.
DC60447	ARV-766	ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].
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).