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2024-07-22Medicilon Events

The Shanghai Overseas Returned Scholars Association invites the Dutch PhD delegation to visit Medicilon, exploring paths for innovative development together

On July 4th, the Shanghai Overseas Returned Scholars Association invited the Dutch PhD delegation to visit the Chuansha campus of Shanghai Medicilon Inc. (Medicilon) and held discussions with Medicilon's Founder and CEO, Chunlin Chen, among others.

2024-07-22Medicilon Events

5th consecutive win! Medicilon once again made the list of "Top 20 Chinese R&D CRO Enterprises in 2024"

Medicilon stood out among hundreds of pharmaceutical enterprises and was honored with the "Top 20 Chinese R&D CRO Enterprises in 2024" award.

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IND 100 Publications

SKLB-YTH-60 ameliorates inflammation and fibrosis in Bleomycin-induced lung fibrosis mouse models. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon

Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through computer-aided drug design, de novo synthesis and high-throughput screening. YTH-60 has obvious anti‐proliferative activity on fibroblasts and A549 cells. YTH-60 has an acceptable oral bioavailability and appropriate eliminated half-life time. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon.

SKLB-YTH-60 ameliorates inflammation and fibrosis in Bleomycin-induced lung fibrosis mouse models. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon

Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 with orally bioavailable and well tolerated in vivo. PK and MTD assays were performed by Medicilon

PROTAC is an attractive technology in drug discovery. Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 which degrades not only ALK or mutant EGFR but also oncoproteins involved in metastasis. SIAIS164018 is orally bioavailable and well tolerated in vivo. Pharmacokinetic and maximal tolerated dose (MTD) assays were performed by Medicilon.

Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 with orally bioavailable and well tolerated in vivo. PK and MTD assays were performed by Medicilon

Discovery and preclinical development of orally active and highly selective follicle stimulating hormone receptor agonists. Toxicological evaluations in both rat and dog were performed by Medicilon

TOP5300 is an orally active follicle stimulating hormone receptor allosteric agonist that provides a preferred treatment for over 16 million infertile women of reproductive age in low complexity methods or in high complexity methods. TOP5300 was evaluated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evaluations were performed in both rat and dog as the second species according to the guidance from FDA. These assays were performed by Medicilon.

Discovery and preclinical development of orally active and highly selective follicle stimulating hormone receptor agonists. Toxicological evaluations in both rat and dog were performed by Medicilon

PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon

Poly ADP-ribose polymerases (PARPs) are a family of enzymes related to DNA damage repair process. Inhibition of PARP1/2 accelerates the damage of injured DNA, which is synthetically lethal to DNA-repairing-deficient cancer cells, such as BRCA1/2-deficient cells. PARP1/2 inhibitors could be a promising candidate for the treatment of cancer. The PARP1 and PARP2 inhibition assays were performed by Medicilon.

PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon

Discovery of STAT3 and HDAC dual-pathway inhibitors for the treatment of solid cancer. The PK experiment in SD Rats was carried out by Medicilon

The inhibition of HDACs will lead to compensated activation of a notorious cancer-related drug target, STAT3, in breast cancer through a cascade, which probably limits the anti-proliferation effect of HDAC inhibitors in solid tumors. Herein, researchers synthesized a series of potent pterostilbene hydroxamic acid derivatives with dual-target inhibition activity. The pharmacokinetic experiment in SD Rats was carried out by Medicilon.

Discovery of STAT3 and HDAC dual-pathway inhibitors for the treatment of solid cancer. The PK experiment in SD Rats was carried out by Medicilon

Apatinib inhibits Paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway

Overexpression of VEGFR2 can offset the rescue effect of Apatinib on Paclitaxel-induced drug resistance of MGC803 cells. Apatinib inhibits Paclitaxel resistance of MGC803 cells via the VEGFR2 signaling pathway. In this research, the VEGFR2 sequences were designed and then amplified by RT-PCR. The sequences were then ligated with a pcDNA3.0 plasmid to construct a recombinant pcDNA3.0-VEGFR2 vector (Medicilon).

Apatinib inhibits Paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway

Researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable

The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification of RNA. Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable, while its enantiomer UZH1b is essentially inactive. The authors thank Medicilon for the synthesis of the UZH1a and UZH1b compounds.

Researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable

Researchers designed and synthesized a photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies were conducted by Medicilon

Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades. In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies of compounds 1 and 2 were conducted by Medicilon. Medicilon's pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody.

Researchers designed and synthesized a photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies were conducted by Medicilon

RIPK2 is an enzyme involved in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase and demonstrates favorable in vitro ADME and PK properties. The PK study was conducted by Medicilon

Receptor interacting protein kinase-2 (RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase (IC50=8 nM) and demonstrates favorable in vitro ADME and pharmacokinetic properties. The pharmacokinetic study was conducted by Medicilon.

RIPK2 is an enzyme involved in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase and demonstrates favorable in vitro ADME and PK properties. The PK study was conducted by Medicilon

Syntheses, biological evaluations, and mechanistic studies of potent PD-L1 inhibitors with in vivo antitumor activity. PK studies were conducted by Medicilon

PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified compound L7 as a potent PD-L1 inhibitor that blocked PD-1/PD-L1 interaction. Pharmacokinetic (PK) studies demonstrated that L7 was orally bioavailable. PK studies were conducted by Medicilon.

Syntheses, biological evaluations, and mechanistic studies of potent PD-L1 inhibitors with in vivo antitumor activity. PK studies were conducted by Medicilon

Global

Address: 20 Maguire Road, Suite 103, Lexington, MA 02421(America)

Tel: +1(626)986-9880(U.S.)

Address: Allia Future Business Centre Kings Hedges Road Cambridge CB4 2HY, UK

Tel: 0044 7790 816 954 (Europe)

Email: marketing@medicilon.com

Address: 5th Floor, 62, Banpodae-ro 4-gil, Seocho-gu, Seoul, 06719 South Korea

Tel: +82 70-8269-5849

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Postcode: 201299

Tel: +86 (21) 5859-1500 (main line)

Fax: +86 (21) 5859-6369

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