MSC-4106 NEW
| Price | $97 | $247 | $397 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: MSC-4106 | CAS No.: 2738542-58-8 |
| Purity: 100% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | MSC-4106 |
| Description | MSC-4106, an orally active and potent YAP/TAZ-TEAD inhibitor, disrupts TEAD1 and TEAD3 auto-palmitoylation and demonstrates significant efficacy in the NCI-H226 tumor xenograft model [1]. |
| In vitro | MSC-4106, at a concentration of 10 μM, demonstrated notable effects in various assays related to cancer cell viability and interaction inhibition within a certain time frame. Specifically, after 24 hours of treatment, it significantly reduced the viability of SK-HEP-1 reporter and NCI-266 cells, with IC50 values measuring at 4 nM and 14 nM, respectively. Additionally, within 6 hours, it was observed to crystalize in the P-site of TEAD1, markedly inhibiting TEAD1 and TEAD3 palmitoylation in TEAD-overexpressing HEK293 cells by 97.3% and 75.9%, correspondingly. A four-day exposure to MSC-4106 also suggested its targeting action on TEAD through a diminished viability in NCI-H226 cells, indicative of its potential mechanistic pathways. Further evaluation via a Cell Viability Assay on NCI-H226 (YAP dependent) and SW620 YAP/TAZ KO (YAP-independent) cells exposed to varying concentrations of MSC-4106 for 96 hours revealed an inhibitory effect on NCI-H226 and a general cytotoxicity towards SW620 with an IC50 greater than 30 μM. Immunofluorescence studies in SK-HEP-1 cells after 24 hours of treatment confirmed the inhibition of YAP-TEAD interaction, showcasing MSC-4106’s multifaceted biochemical activities. |
| In vivo | MSC-4106 (P.O.; 100 mg/kg once daily; 7 days) demonstrates anti-tumor effects with controlled tumor volume and good tolerability, maintaining stable body weight in mice [1]. MSC-4106 (P.O.; 1, 5, 100 mg/kg once daily; 6, 24, 30, 48, and 72 h) down-regulates Cyr61 (cysteine-rich angiogenic inducer 61) expression, a TEAD-regulated target gene, in tumor lysates at all time points at 100 mg/kg and at 24 h at 5 mg/kg [1]. Pharmacokinetic (PK) profiles in different species [1]: - Mouse: Cl (0.2 l/h/kg), PO t 1/2 (45 h), PO AUC (45 μg h/mL), V ss (2 L/kg), F (>90%). - Rat: Cl (0.7 l/h/kg), PO t 1/2 (40 h), PO AUC (10 μg h/mL), V ss (5 L/kg), F (80%). - Dog: Cl (0.05 l/h/kg), PO t 1/2 (3.6 h), PO AUC (33 μg h/mL), V ss (0.3 L/kg), F (18%). Note: PO studies at 10 mg/kg; MSC-4106 formulated in 20% Kleptose in 50 mM PBS, pH 7.4. Animal model: NCI-H226 xenograft in H2d Rag2 female mice (9-week-old) [1]. Dosage: 5, 100 mg/kg Oral gavage, once daily for 32 days, resulting in controlled tumor growth at 5 mg/kg and tumor regression at 100 mg/kg after 32 days of treatment. |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 225 mg/mL (626.2 mM), Sonication is recommended. |
| Keywords | MSC4106 | MSC-4106 | MSC 4106 |
| Inhibitors Related | AICAR | MY-1076 | YAP-TEAD-IN-3 | DC-TEADin02 | Verteporfin | Lats-IN-1 | VT103 | VT107 | ML-7 hydrochloride | PY-60 | VT104 | MYF-01-37 |
| Related Compound Libraries | Bioactive Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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