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MD-224

  Cat. No.:  DC28018   Featured
Chemical Structure
2136247-12-4
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More than 5000 active chemicals with high quality for research!
Field of application
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2136247-12-4
Chemical Name: MD-224
Synonyms: MD-224 ,MD 224 ,MD224
SMILES: FC1C([C@H]2[C@H](C(=O)NC3C=CC(C(=O)NCCCC#CC4C=CC=C5C(=O)N(C6CCC(=O)NC6=O)CC=45)=CC=3)NC3(CCCCC3)[C@]32C(=O)NC2C=C(Cl)C=CC3=2)=CC=CC=1Cl
Formula: C48H43Cl2FN6O6
M.Wt: 889.79
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
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).
DC53120 XD2-149 XD2-149 is a napabucasin PROTAC as an effective degrader of the E3 ligase ZFP91 with IC50 of 1 μM and 0.8 μM in pancreatic cancer cell lines, MIA PaCa-2 and BxPC-3, respectively. XD2-149 also reduces the expression of STAT3, pSTAT3, and NQO1 proteins.
DC51010 CID 138454799 ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
DC31014 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein[1].
DC28018 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
DC12022 dBET6 dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.
DC12023 dBET1 dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
DC12380 BSJ-03-123 BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.
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