MSC-4106 |
Catalog No.GC65993
One-Click Copy Product Info
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MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2738542-58-8
Sample solution is provided at 25 µL, 10mM.
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MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model[1].
MSC-4106 (10 μM, 24 h) inhibited SK-HEP-1 reporter and NCI-266 cell viability with IC50 values of 4 nM and 14 nM, respectively[1].
MSC-4106 (10 μM, 6 h) crystallizes in the P-site of TEAD1, and against TEAD1 or TEAD3 palmitoylation in TEAD-Overexpressing HEK293 Cells by 97.3% and 75.9%, respectively[1].
MSC-4106 (10 μM, 4 d) targets TEAD indicated by a reduction in viability of NCI-H226 cells[1].
Cell Viability Assay[1]
| Cell Line: | NCI-H226 (YAP dependent); SW620 YAP/TAZ KO (Yap-independent) cells |
| Concentration: | 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM |
| Incubation Time: | 96 hours |
| Result: | Showed inhibitory effect to NCI-H226 and general cytotoxic to SW620 (IC50 >30 μM). |
Immunofluorescence[1]
| Cell Line: | SK-HEP-1 |
| Concentration: | 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited YAP-TEAD interation. |
MSC-4106 (100 mg/kg/d; p.o.; 7 d) displays anti-tumor effect with controlled tumor volume and good tolerability with stable body weight in mice[1].
MSC-4106 (1, 5, 100 mg/kg/d; p.o.; 0-72 h) down-regulates Cyr61 (cysteine-rich angiogenic inducer 61) expression, the TEAD-regulated target gene, in tumor lysates at all time points at 100 mg/kg and 24 h at 5 mg/kg[1].
Pharmacokinetics (PK) profile in different species[1]
| Parameter | Mouse | Rat | Dog |
| Cl (l/h/kg) | 0.2 | 0.7 | 0.05 |
| PO t1/2 (h) | 45 | 40 | 3.6 |
| PO AUC (μg•h/mL) | 45 | 10 | 33 |
| Vss (L/kg) | 2 | 5 | 0.3 |
| F (%) | >90 | 80 | 18 |
| Animal Model: | NCI-H226 xenograft model in H2d Rag2 female mice (9-week-old)[1] |
| Dosage: | 5, 100 mg/kg |
| Administration: | Oral gavage; once daily; 32 days |
| Result: | Resulted tumor growth controlled with 5 mg/kg while regressed with 100 mg/kg dosing after 32 treatment days. |
| Cas No. | 2738542-58-8 | SDF | |
| Formula | C18H12F3N3O2 | M.Wt | 359.3 |
| Solubility | DMSO : 250 mg/mL (695.80 mM; Need ultrasonic) | Storage | Store at -20°C, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7832 mL | 13.9159 mL | 27.8319 mL |
| 5 mM | 556.6 μL | 2.7832 mL | 5.5664 mL |
| 10 mM | 278.3 μL | 1.3916 mL | 2.7832 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)