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PROTAC R&D Service Platform

PROTAC R&D Service Platform

Deeply integrate R&D experience, constantly climb the peak of R&D technology, and build an integrated innovation service platform for new drug R&D.

PROTAC R&D Service Platform

Medicilon has obtained popular POI ligands and multiple E3 ligase ligands and hasestablished a linker library containing hundreds of distinct linking molecules.
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Medicilon diamond icon.pngPROTAC technology has a unique mechanism
Medicilon diamond icon.pngAdvantages of PROTAC in Drug Development
Medicilon diamond icon.pngIntroduction of Medicilon PROTAC Services
  • In Vitro Screening of PROTAC-POI
    Cytotoxicity Assay (CCK-8 & CTG)
    Mechanism detection by proliferation inhibition tests.

    Percentage-degradation-of-HiBiT-IRAK4-in-HiBiT-IRAK4-overexpression-OCI-LY10-cells.png

    Percentage degradation of HiBiT-IRAK4 in HiBiT-IRAK4 overexpressing OCI-LY10 cells

    Western Blot(WB)
    We conduct WB to test the target proteins degradation ability and to analyze DC50.

    Western-blot-of-anti-IRAK4-on-OCI-LY10-cells-treated-with-IRAK4-degrader-1.png

    Western blot of anti-IRAK4 on OCI-LY10 cells treated with IRAK4 degrader-1

    Pomalidomide-(CRBN-binder)-competition-experiment-show-that-IRAK4-degrader-1--degrades-IRAK4-through-CRBN.png

    Pomalidomide (CRBN binder) competition experiment show that IRAK4 degrader-1  degrades IRAK4 through CRBN

    MG132-inhibition-experiment-show-that-IRAK4-degrader-1-degrades-IRAK4-through-proteasome-pathway.png

    MG132 inhibition experiment show that IRAK4 degrader-1 degrades IRAK4 through proteasome pathway

    Tumor cell proliferation inhibition effect test

    Growth-inhibition-effect-of-IRAK4-degrader-1-on-OCI-LY10-cells.png

    Growth inhibition effect of IRAK4 degrader-1 on OCI-LY10 cells

    ACBI1-(BRM-degrader)-degrades-BRM-in-dose-response-manner.png

    ACBI1 (BRM degrader) degrades BRM in a dose-dependent manner

  • Validated PROTAC Targets and Assays
    Validated PROTACsTargetsValidated assay
    MP-A001IRAK4IRAK4 kinase assay; OCI-LY10 cytotoxicity assay; Western blot-based degradation assay; HiBiT-IRAK4 degradation assay (OCI-LY10 cells); HTRF-based    IRAK4 degradation assay
    ARV-110ARWestern-based assay degradation assay; LNCAP cytotoxicity assay; AR depende nt MDA-KB-2 cell reporter assay
    FulvestrantERWestern-based assay degradation assay; MCF-7 cytotoxicity assay; ER dependent MDA-KB-2 cell reporter assay
    LenalidomideIKZF1Western-based assay degradation assay; ln-cell Western-based degradation assay
    LenalidomideIKZF3Western-based assay degradation assay; ln-cell Western-based degradation assay
    PROTAC-3EGFREGFR kinase assay(EGFR-WT and mutants); Western-based degradation assay;NCI-H1975,HCC827 cytotoxicity assay; EGFR-HiBiT assay(HEK293 cells)
    BSJ-04-132CDK4CDK4 kinase assay; Western-based degradation assay; HiBiT-CDK4 degaradation assay; Cytotoxicity assay
    BSJ-04-132CDK6CDK6 kinase assay; Western-based degradation assay; HiBiT-CDK6 degaradation assay; Cytotoxicity assay
    ACBI-2SMARCA2BRD domain binding assay; Western-based degradation assay; HiBiT-SMARCA2 degradation assay; MV-4-11 cytotoxicity assay
    ACBI-2SMARCA4BRD domain binding assay; Western-based degradation assay; HiBiT-SMARCA4 degradation assay
    PROTAC KRAS  G12C degrader-1KRAS G12CKRAS G12C/S0S1 binding assay; Western-based degradation assay
  • In Vivo Efficacy Tests of PROTAC-POI
    CDX Mouse Tumor Model

    Cancer TypeOrthotopic ModelOrthotopic Model (Luc Cell Line)
    Brain CancerU87-MGU87-MG-luc
    Lung CancerNCI-H1650, A549, NCI-H1975, NCI-H460, LLC1A549-luc, LLC1-luc,NCI-H1975-luc
    Colon CancerHCT-116, LoVoHT29-luc
    Gastric CancerHs 746T
    Pancreas CancerMia-Paca 2Mia-Paca 2-luc
    Breast CancerMDA-MB-2314T1-luc
    Ovarian CanerSK-OV-3SK-OV-3-luc
    Prostate CancerPC3PC-3-luc
    Renal CancerA498
    Bladder CancerUM-UC-3
    MelanomaB16-F10-luc
    Liver CancerH22
    Bone Cancer
    PDX Mouse Tumor Model

    Cancer TypeCell Lines
    Colon Cancer                                PDXM-008C, PDXM-016C, PDXM-020C, PDXM-021C, PDXM-057C, PDXM-060C,    PDXM-075C, PDXM-076C, PDXM-087C, PDXM-104C, PDXM-095C, PDXM-084C, PDXM-072C,    PDXM-069C, PDXM-057C, PDXM-015C, PDXM-002C,
    Lung Cancer                                PDXM-054Lu, PDXM-050Lu, PDXM-047Lu, PDXM-053Lu, PDXM-028Lu,
    Gastric CancerPDXM-092Ga, PDXM-091Ga,
    Breast CancerPDXM-201B, PDXM-202B, PDX-203B
    Liver CancerPDXM-211Li, PDXM-212Li
    Pancreas CancerPDXM-221Pa, PDXM-222Pa
    Bladder CancerPDXM-231U, PDXM-232U
    LymphomaPDXM-241Ly, PDXM-242Ly
  • Integrated Preclinical Services
    We can further characterise PROTAC molecules by using our integrated preclinical services including PK/PD studies, pharmacological analysis, pharmacokinetic studies, and safety evaluation.
    The pharmacokinetics (PK) data show that five highly potent androgen receptor (AR) degraders achieve good to excellent overall PK profiles with ARD-2128 being the best compound. ARD-2128 has low clearance (1.2 mL/min/kg) and a moderate to high steady-state volume of distribution (Vss) of 2.7 L/kg. ARD-2128 (2 mg/kg, i.v.) and ARD-2128 (5 mg/kg, p.o.) both have long half-lives following intravenous and oral administration with the T1/2s of 27.6 h and 18.8 h, respectively. ARD-2128 (5 mg/kg) achieves 67% oral bioavailability in mice, effectively reduces AR protein and suppresses AR-regulated genes in tumor tissues with oral administration, leading to the effective inhibition of tumor growth in mice without signs of toxicity.
     Summary of PK Data for Five Compounds in Male ICR Mice
    Summary of PK Data for Five Compounds in Male ICR Mice[1]
    The plasma and microsomal stability data show that ARD-2128 has excellent plasma and microsomal stability in in mouse, rat, dog, monkey, and humans.
    Evaluation of ARD-2128 for Its Plasma Stability and Microsomal Stability
    Evaluation of ARD-2128 for Its Plasma Stability and Microsomal Stability[1]
    References:
    [1].Xin Han,et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer.J Med Chem. 2021 Sep9;64(17):12831-12854. doi: 10.1021/acs.jmedchem.1c00882. Epub 2021 Aug
Service Cases

Signing Ceremony for Strategic Cooperation Between Gluetacs and Medicilon IND R&D Service.webp

Signing Ceremony for Strategic Cooperation Between Gluetacs and Medicilon IND R&D Service

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Medicilon Assists | Cullgen's class 1 new drug TRK degrader CG001419 was approved for clinical use.webp

Medicilon Assists | Cullgen's class 1 new drug TRK degrader CG001419 was approved for clinical use

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 CGeneTech and Medicilon Held the Conference Titled PROTAC Project Contract Signing & Kick-off Meeting.webp

CGeneTech and Medicilon Held the Conference Titled "PROTAC Project Contract Signing & Kick-off Meeting"

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  • BD-FACSCelesta-Flow cytometer - 12 channels
  • triple-quad-7500
  • eppendorf-centrifuge-5810R
  • Spectra-MaxM2
  • BD-FACSymphoy-A3
  • hydro
  • Sciex-Triple-Quad-6500-Waters-ACQUITY-UPLC
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  • Biological sample homogenizer
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  • bio-Plex-200-and-Gyrolab
  • Sciex-Triple-Quad6500-LC-30AD
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