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HomeClient CenterMedicilon SupportPublications
IND 100 Publications
Jul 11,2023
Tankyrase 1/2 impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer
Tankyrase 1 and 2 (TNKS1/2) impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer. OM-153 shows picomolar IC50 inhibition in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable ADME properties, and an improved pharmacokinetic profile in mice. The pharmacokinetic analyses in mice were performed according to the standard protocols of Medicilon.
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Tankyrase 1/2 impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer
Jul 11,2023
Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon
Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Researchers designed 1-(Indolizin-3-yl)ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer. Pharmacokinetic properties evaluation were analyzed by Medicilon. Liver microsomal stability assay were performed at Medicilon. Caco-2 permeability assay was analyzed by Medicilon.
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Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon
Jul 11,2023
Researchers used RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. RZ-2994 was obtained from Medicilon
Despite progress in the treatment of T-cell acute lymphoblastic leukemia (T-ALL) has limited treatment options, particularly in the setting of relapsed/refractory disease. Researchers used SHMT1/2 inhibitor RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. Loss of both SHMT1/2 is necessary for impaired growth and cell cycle arrest, with suppression of SHMT1/2 inhibiting leukemia progression. RZ-2994 also decreases leukemia burden in vivo. RZ-2994 was obtained from Medicilon. Medicilon offers a full range of chemical services covering all phases of your project. Cus-tomers can work with us either through FFS or FTE.
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Researchers used RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. RZ-2994 was obtained from Medicilon
Jul 11,2023
Researchers developed a highly specific CDC7 inhibitor TAK-931 as a clinical cancer therapeutic agent. The antitumor efficacy studies were performed at Medicilon
Cell division cycle 7 (CDC7) plays important roles in DNA replication. Researchers developed a highly specific CDC7 inhibitor, TAK-931, as a clinical cancer therapeutic agent. The antitumor efficacy studies in PDX models were performed at Medicilon. Medicilon has established a complete evaluation system for preclinical anti-tumor efficacy, and has more than 200 different types of tumor efficacy models.
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Researchers developed a highly specific CDC7 inhibitor TAK-931 as a clinical cancer therapeutic agent. The antitumor efficacy studies were performed at Medicilon
Jul 11,2023
Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agent. The binding inhibition activities of MT-1207 were evaluated by Medicilon
Hypertension is a serious public health problem worldwide. MT-1207 is a chemical entity that has entered into clinical trial as antihypertensive agent. MT-1207 potently inhibits adrenergic α1A, α1B, α1D, and 5-HT2A receptors with Ki < 1 nM in a panel of enzyme activity or radioligand binding assays. The binding inhibition activities of MT-1207 were evaluated by Medicilon.
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Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agent. The binding inhibition activities of MT-1207 were evaluated by Medicilon
Jul 11,2023
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).
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Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
Jul 11,2023
Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.
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Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
Jul 11,2023
Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon
Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.
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Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon
Jul 11,2023
ARD-2585 is an orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
A PROTAC-based androgen receptor (AR) degrader is a bifunctional small molecule, consisting of an AR ligand that binds to AR protein, and a ligand that binds to and recruits an E3 ligase complex, tethered together through a linker. Researchers report the discovery of exceptionally potent and orally bioavailable PROTAC AR degrader ARD-2585 (Compound 43). ARD-2585 is a promising AR degrader for extensive investigations for the treatment of advanced prostate cancer. The liver microsomal stability assay was performed by Medicilon. The plasma stability assay was performed by Medicilon. The hERG assay was performed by Medicilon.
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ARD-2585 is an orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
Jul 11,2023
A selective c-Myc degrader potently regresses lethal c-Myc overexpressing tumors. SPR experiments were performed by Medicilon
Cancer is one of the leading causes of death worldwide. MYC oncogene is involved in the majority of human cancers and is often associated with poor outcomes. WBC100, a novel oral active molecule glue that selectively degrades c‐Myc protein over other proteins and potently kills c‐Myc overexpressing cancer cells is reported. Researchers performed direct binding assay of WBC100 with c-Myc on biosensor chip by surface plasmon resonance (SPR). SPR experiments were performed using a Biacore T200 instrument by Medicilon.
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A selective c-Myc degrader potently regresses lethal c-Myc overexpressing tumors. SPR experiments were performed by Medicilon
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