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| 1mg |
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| 5mg |
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| Targets |
SRI31215 2TFA is a triplex inhibitor of matriptase, hepsin, and HGFA (hepatocyte growth factor activator). It mimics the activity of HAI-1/2, endogenous inhibitors of these proteases. By inhibiting matriptase, hepsin, and HGFA, SRI31215 2TFA blocks signaling between cancer cells and fibroblasts and inhibits the tumor-promoting activity of cancer-associated fibroblasts. Its mechanism involves inhibition of these proteases, which are involved in cancer progression.
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| ln Vitro |
SRI 31215 (TFA) exhibits strong anti-matriptase, anti-hepsin, and anti-HGFA properties, with IC50 values of 0.69 μM, 0.65 μM, and 0.30 μM, in that order[1]. Pro-HGF's activation by protein flipping is blocked by SRI 31215 (10 μM) [1]. In tumor cells, fibroblast-induced HGF/MET signaling is transcribed by SRI 31215 (10 μM, 30 min) [1]. The epithelial-mesenchymal transition in tumor cells triggered by transcriptional fibroblasts (SRI 31215 (10 μM) overcomes the autonomous HGF/MET signaling-mediated avoidance of EGFR in SAD [1]. 72-hour SRI31215 (10 μM) integration
In vitro, SRI31215 2TFA has IC50 values of 0.69 µM, 0.65 µM, and 0.30 µM for matriptase, hepsin, and HGFA, respectively. It blocks signaling between cancer cells and fibroblasts. Its in vitro activity is characterized by potent inhibition of matriptase, hepsin, and HGFA, and modulation of cancer-stromal interactions. SRI31215 2TFA is a novel and potent triplex inhibitor. |
| ln Vivo |
In vivo, SRI31215 2TFA inhibits the tumor-promoting activity of cancer-associated fibroblasts. It has potential applications in cancer research. However, detailed in vivo efficacy data for specific disease models are limited. SRI31215 2TFA is primarily used as a research tool for studying matriptase, hepsin, and HGFA biology and cancer.
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| Enzyme Assay |
In vitro enzyme assays for SRI31215 2TFA typically involve measuring the inhibition of matriptase, hepsin, and HGFA protease activities. The compound has IC50 values of 0.69 µM, 0.65 µM, and 0.30 µM for matriptase, hepsin, and HGFA, respectively. These assays confirm its mechanism of action as a triplex protease inhibitor.
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| Cell Assay |
Western blot analysis [1]
Cell Types: DU145 Cell Tested Concentrations: 10 μM Incubation Duration: 30 minutes Experimental Results: Prevents fibroblast-induced MET activation and signaling by anti-EGFRi-induced Cell-mediated resistance [1]. Tumor cells, but cannot prevent active HGF-induced MET activation. Cell migration assay [1] Cell Types: DU145 Cell Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Does not interfere with HGF-induced MET activation migration, but inhibited fibroblast-induced migration of DU145 cells. In vitro cellular assays for SRI31215 2TFA typically involve treating cancer cells and fibroblasts with the compound and measuring signaling between cancer cells and fibroblasts. The compound blocks signaling between cancer cells and fibroblasts and inhibits the tumor-promoting activity of cancer-associated fibroblasts. These cell-based studies demonstrate its functional inhibition of protease activity and its effects on cancer-stromal interactions. |
| ADME/Pharmacokinetics |
SRI31215 2TFA has a molecular weight of 647.61 and a molecular formula of C29H35F6N5O5. Its CAS number is 1832686-44-8. The compound is the di-trifluoroacetic acid salt of SRI31215. It is a novel and potent triplex inhibitor of matriptase, hepsin, and HGFA. SRI31215 2TFA mimics the activity of HAI-1/2.
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| Toxicity/Toxicokinetics |
SRI31215 2TFA is a triplex protease inhibitor with a well-characterized mechanism of action. As with any protease inhibitor, potential toxicity may include effects on normal protease function and tissue remodeling. The compound's safety profile should be evaluated in preclinical toxicology studies. SRI31215 2TFA is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying matriptase, hepsin, and HGFA biology and cancer.
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| References | |
| Additional Infomation |
SRI31215 2TFA (CAS# 1832686-44-8) is a novel and potent triplex inhibitor of matriptase, hepsin, and HGFA. It has IC50 values of 0.69 µM, 0.65 µM, and 0.30 µM for matriptase, hepsin, and HGFA, respectively. SRI31215 2TFA mimics HAI-1/2 activity and inhibits tumor-promoting activity of cancer-associated fibroblasts. The compound is for research use only and not for human therapeutic use.
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| Molecular Formula |
C27H34F3N5O3
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| Molecular Weight |
533.585776805878
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| Exact Mass |
533.261
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| CAS # |
1832686-44-8
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| Related CAS # |
1832686-44-8 (2TFA);1832686-43-7;
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| PubChem CID |
102004307
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| Appearance |
Light yellow to khaki solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
38
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| Complexity |
695
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C(=O)O)(F)F.O=C1N(C2C=CC=C(C(=N)N)C=2)CC(C)CN1CC1CCN(CC2C=CC=CC=2)CC1
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| InChi Key |
QJFJKJLPPLYFJA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H33N5O.C2HF3O2/c1-19-15-29(25(31)30(16-19)23-9-5-8-22(14-23)24(26)27)18-21-10-12-28(13-11-21)17-20-6-3-2-4-7-20;3-2(4,5)1(6)7/h2-9,14,19,21H,10-13,15-18H2,1H3,(H3,26,27);(H,6,7)
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| Chemical Name |
3-[3-[(1-benzylpiperidin-4-yl)methyl]-5-methyl-2-oxo-1,3-diazinan-1-yl]benzenecarboximidamide;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~234.26 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8741 mL | 9.3705 mL | 18.7410 mL | |
| 5 mM | 0.3748 mL | 1.8741 mL | 3.7482 mL | |
| 10 mM | 0.1874 mL | 0.9370 mL | 1.8741 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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