| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
| Targets |
RON (IC50 = 9 nM)
|
|---|---|
| ln Vitro |
SYN1143 (Compound I) (10-1000 nM; 1 h) suppresses HT-29 and BxPC3 cells' functional activity and c-Met-mediated signaling[1].
SYN1143 (10-1000 nM; 1 h) suppresses NIH3T3 RON and BxPC3 cells' RON-mediated signaling and functional activity[1]. SYN1143 (0.3-30 μM; 2 h or 3 d) suppresses c-Met signaling and cell proliferation in MC3T3-E1 and C3H10T1/2 cells[2]. SYN1143 (0.3-2 μM; 4-12 d) increases precursor cell osteogenic differentiation [2]. |
| ln Vivo |
SYN1143 (10-100 mg/kg; p.o. for 22 d) suppresses the growth of RON-expressing tumors that are constitutively active and c-Met-dependent[1].
SYN1143 (20-50 μg; transferred into calvarial defects) promotes the growth of new bone in mouse calvarial bone defects of critical size[2]. |
| Animal Protocol |
Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s.c. tumors[1]
10, 30, 100 mg/kg Oral gavage either once or twice daily for 22 days |
| References |
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| Additional Infomation |
N-[3-fluoro-4-[(7-methoxy-4-quinolinyl)oxy]phenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-4-pyrazolecarboxamide is an aromatic amide.
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| Molecular Formula |
C31H29FN4O4
|
|---|---|
| Molecular Weight |
540.59
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| Exact Mass |
556.212
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| Elemental Analysis |
C, 68.88; H, 5.41; F, 3.51; N, 10.36; O, 11.84
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| CAS # |
913376-84-8
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| Related CAS # |
913376-84-8
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| PubChem CID |
16757524
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.660
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| LogP |
4.39
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
41
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| Complexity |
986
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=C(C)N(CC(C)(C)O)N(C2C=CC=CC=2)C1=O)NC1C=C(F)C(OC2C3C(=CC(=CC=3)OC)N=CC=2)=CC=1
|
| InChi Key |
UYMSIPINLJNNOU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H29FN4O5/c1-19-28(30(38)36(21-8-6-5-7-9-21)35(19)18-31(2,3)39)29(37)34-20-10-13-27(24(32)16-20)41-26-14-15-33-25-17-22(40-4)11-12-23(25)26/h5-17,39H,18H2,1-4H3,(H,34,37)
|
| Chemical Name |
N-[3-fluoro-4-(7-methoxyquinolin-4-yl)oxyphenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide
|
| Synonyms |
RON-IN-1; RONIN1; RON inhibitor 1; RON IN 1; Met Kinase Inhbitor IV ; RON inhibitor-1; Ron Inhibitor I
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (179.7 mM)
Ethanol: ~60 mg/mL (107.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (4.49 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 25.0 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: ≥ 2.5 mg/mL (4.49 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 | 1.8498 mL | 9.2492 mL | 18.4983 mL | |
| 5 mM | 0.3700 mL | 1.8498 mL | 3.6997 mL | |
| 10 mM | 0.1850 mL | 0.9249 mL | 1.8498 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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