SYN1143
Based on 1 Customer Validation
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.07%
- No. CAS: 913376-84-8
- Fòrmula: C31H29FN4O5
- Peso molecular:556.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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RON 9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
921 nM
Compound: 7
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Inhibition VEGFR2-mediated survival of HUVEC
Inhibition VEGFR2-mediated survival of HUVEC
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[PMID: 18553959] |
| PC-3 | IC50 |
50 nM
Compound: 7
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Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells
Inhibition of HGF-mediated c-Met phosphorylation in human PC3 cells
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[PMID: 18553959] |
| PC-3 | IC50 |
50.5 nM
Compound: 58e
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Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
Inhibition of HGF-mediated c-Met autophosphorylation in human PC3 cells after 10 mins by quantitative electrochemiluminescent immunoassay
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[PMID: 22320327] |
SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells[1].
SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells[1].
SYN1143 (0.3-30 μM; 2 h or 3 d) inhibits c-Met signaling and cell proliferation in MC3T3-E1 and C3H10T1/2 cells[2].
SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 and BxPC3 cells
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Concentration:10, 30, 100, 300, 1000 nM
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Incubation Time:1 hours
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Result:Inhibited HGF-mediated c-Met phosphorylation and downstream signaling in a dose-dependent manner in both cell lines.
SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s.c. tumors[1]
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Dosage:10, 30, 100 mg/kg
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Administration:Oral gavage either once or twice daily for 22 days
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Result:Significantly inhibited tumor growth at doses of 30 or 100 mg/kg once daily or at 30 mg/kg twice daily.
Completely inhibited tumor growth at a dose of 100 mg/kg once daily.
Did not adversely affect body weight.
Chemical Information
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No. CAS 913376-84-8
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Appearance Solid
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Peso molecular 556.58
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Fòrmula C31H29FN4O5
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Color Light yellow to yellow
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SMILES
O=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=CC=C(OC4=CC=NC5=CC(OC)=CC=C45)C(F)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (179.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhang Y, et, al. Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7. [Content Brief]
[2]. Kim JW, et, al. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur J Pharmacol. 2017 Jul 5;806:10-17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7967 mL | 8.9834 mL | 17.9669 mL | 44.9172 mL |
| 5 mM | 0.3593 mL | 1.7967 mL | 3.5934 mL | 8.9834 mL | |
| 10 mM | 0.1797 mL | 0.8983 mL | 1.7967 mL | 4.4917 mL | |
| 15 mM | 0.1198 mL | 0.5989 mL | 1.1978 mL | 2.9945 mL | |
| 20 mM | 0.0898 mL | 0.4492 mL | 0.8983 mL | 2.2459 mL | |
| 25 mM | 0.0719 mL | 0.3593 mL | 0.7187 mL | 1.7967 mL | |
| 30 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4972 mL | |
| 40 mM | 0.0449 mL | 0.2246 mL | 0.4492 mL | 1.1229 mL | |
| 50 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL | |
| 60 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7486 mL | |
| 80 mM | 0.0225 mL | 0.1123 mL | 0.2246 mL | 0.5615 mL | |
| 100 mM | 0.0180 mL | 0.0898 mL | 0.1797 mL | 0.4492 mL |
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