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IND 100 Publications
Jul 11,2023
TAK-243 is a potent ubiquitin activating enzyme inhibitor with antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 model
The ubiquitin–proteasome system (UPS) comprises a network of enzymes that is responsible for maintaining cellular protein homeostasis. TAK-243 is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade. TAK-243 has UAE-specific antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 (triple-negative breast cancer) model.
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TAK-243 is a potent ubiquitin activating enzyme inhibitor with antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 model
Jul 11,2023
Farnesyltransferase inhibitor LNK-754 could rapidly cross the blood-brain-barrier after a single oral dose. Pharmacokinetic analysis was performed by Medicilon
Age-related neurodegenerative disorders are characterized by the progressive accumulation of misfolded and aggregated proteins. SNARE protein ykt6 plays a crucial role in proteostasis and lysosomal function by enhancing hydrolase trafficking under stressful conditions. Activating ykt6 by small-molecule farnesyltransferase inhibitors (FTIs) restores lysosomal activity and reduces a-synuclein in patient-derived neurons and mice. Pharmacokinetic studies revealed that after a single oral dose, the FTI (LNK-754) was cleared from plasma within 20 hours and could rapidly cross the blood-brain-barrier. Pharmacokinetic analysis was performed as a service provided by Medicilon.
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Farnesyltransferase inhibitor LNK-754 could rapidly cross the blood-brain-barrier after a single oral dose. Pharmacokinetic analysis was performed by Medicilon
Jul 11,2023
WYC-209 inhibits proliferation of malignant murine melanoma tumor-repopulating cells. SPR analysis was carried out by Medicilon, using the Biacore 8K equipment
​Developing novel drugs that can abrogate the growth and metastasis of malignant tumors is a major challenge for cancer researchers. WYC-209, a synthetic retinoid, inhibits proliferation of malignant murine melanoma tumor-repopulating cells (TRCs). The enantiomers WYC-209A and WYC-209B exhibit similar TRC inhibition activities. The binding assay by surface plasmon resonance (SPR) analysis shows that WYC-209A and WYC-209B acid bind to RARs at nano-molar doses. SPR was carried out by Medicilon, using the Biacore 8K equipment.
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WYC-209 inhibits proliferation of malignant murine melanoma tumor-repopulating cells. SPR analysis was carried out by Medicilon, using the Biacore 8K equipment
Jul 11,2023
ARD-2128 is a PROTAC AR degrader with excellent plasma and microsomal stability. The in vitro stability and PK studies were performed by Medicilon
ARD-2128 is a bona fide PROTAC androgen receptor (AR) degrader and strongly suppresses AR-regulated genes in a dose- and time-dependent manner in AR+ prostate cancer cell lines. ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.
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ARD-2128 is a PROTAC AR degrader with excellent plasma and microsomal stability. The in vitro stability and PK studies were performed by Medicilon
Jul 11,2023
A series of DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents are designed and synthesized. The PK study was conducted by Medicilon
​Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases. Herein, researchers designed and synthesized a series of acrylamide-based novel DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents. The most potent compound 54 displays favorable pharmacokinetic (PK) profiles in vivo. The PK study was conducted by using Medicilon's preclinical.
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A series of DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents are designed and synthesized. The PK study was conducted by Medicilon
Jul 11,2023
A new LC-MS/MS method for the simultaneous quantification of Dabrafenib and its main metabolite hydroxy-dabrafenib (OHD) in human plasma has been developed and validated
Increased understanding of molecular pathways leads to the development of effective targeted therapies for the treatment of solid tumors. Dabrafenib (DAB) undergoes oxidative metabolism via cytochrome P450 (CYP) 3A4 and CYP2C8 to form hydroxy-dabrafenib (OHD), an active metabolite, with a twofold higher potency than an inhibitor of mutant BRAF. OHD (purity>99 %) was synthesized by Medicilon. Medicilon synthetic chemistry team is capable of the independent design of synthesis pathways and complex compound treatments, key to helping accelerate drug discovery.
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A new LC-MS/MS method for the simultaneous quantification of Dabrafenib and its main metabolite hydroxy-dabrafenib (OHD) in human plasma has been developed and validated
Jul 11,2023
Radiation therapy is used as the primary treatment for lung cancer. In this study, radiation therapy for establish ionizing radiation-resistant lung cancer cell lines was supported by Medicilon
Radiation therapy is used as the primary treatment for lung cancer. In this study, radiation therapy for establish ionizing radiation-resistant lung cancer cell lines (A549-IR/H1299-IR) was supported by Medicilon. The A549 and H1299 cells in exponential growth phase were treated with a repeated IR dose of 2 Gy each at room temperature and then returned to the incubator.
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Radiation therapy is used as the primary treatment for lung cancer. In this study, radiation therapy for establish ionizing radiation-resistant lung cancer cell lines was supported by Medicilon
Jul 11,2023
CAR-T has shown promising clinical results in the treatment of leukemia and lymphoma. The shRNA vector plasmid that silences PD-1 and preparation of CAR is constructed. The plasmids sequenced were fully identified by Medicilon
Chimeric antigen receptor T cells (CAR-T) immunotherapy has shown promising clinical results in the treatment of leukemia and lymphoma, but the effectiveness is limited for solid tumors. The shRNA vector plasmid that silences PD-1 and preparation of CAR is constructed. The plasmids sequenced were fully identified by Medicilon.
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CAR-T has shown promising clinical results in the treatment of leukemia and lymphoma. The shRNA vector plasmid that silences PD-1 and preparation of CAR is constructed. The plasmids sequenced were fully identified by Medicilon
Jul 11,2023
Amorphous solid dispersion of Sorafenib was used to develop an immediate release tablet with improved oral bioavailability. The PK study was performed by Medicilon
An amorphous solid dispersion (ASD) of Sorafenib (SOR) was used to develop an immediate release tablet with improved oral bioavailability. The SOR ASD tablets exhibited approximately 50% higher relative bioavailability in dogs than the marketed SOR tablet product, Nexavar®. The pharmacokinetic (PK) study of SOR ASD tablets and Nexavar® tablets was performed by Medicilon.
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Amorphous solid dispersion of Sorafenib was used to develop an immediate release tablet with improved oral bioavailability. The PK study was performed by Medicilon
Jul 11,2023
TAK-931 is a highly specific CDC7 inhibitor with antitumor efficacy and immunity. In vivo efficacy studies were performed at Medicilon
Cell division cycle 7 (CDC7), a serine/threonine kinase, plays important roles in the initiation of DNA replication. TAK-931, a highly specific CDC7 inhibitor, exhibits antitumor efficacy and immunity. The flowcytometry-based immune profiling panel studies in J558 allograft syngeneic mouse models were performed at Medicilon. In vivo efficacy studies in J558 allograft models in combination with anti-mPD-1, anti-mPD-L1, and anti-mCTLA-4 antibodies were performed at Medicilon.
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TAK-931 is a highly specific CDC7 inhibitor with antitumor efficacy and immunity. In vivo efficacy studies were performed at Medicilon
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