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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
BMS-794833 (BMS794833; BMS 794833) is an ATP competitive multi-kinase (Met/VEGFR2) inhibitor with potential anticancer activity. It has IC50s of 1.7 nM and 15 nM for Met/VEGFR2 inhibition, respectively. In both an in vivo and in vitro model of human gastric tumor xenografts and U87 glioblastoma, BMS-794833 exhibits strong anti-proliferative activity and antitumor efficacy.
| Targets |
VEGFR2 (IC50 = 15 nM); Met (IC50 = 1.7 nM)
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| ln Vitro |
BMS794833 inhibits the Met receptor-activated gastric carcinoma cell line, GTL-16, with an IC50 of 39 nM[1].
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| ln Vivo |
BMS-794833 is active by more than 50% tumor growth inhibition for at least one tumor doubling time in the GTL-16 gastric carcinoma model. When given once daily for a total of 14 days, no toxicity is seen at any of the dose levels[1].
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| Enzyme Assay |
BMS798433 is dissolved in DMSO and diluted by water before use. The reaction mixture includes 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1 mg BSA, 0.1 mg polyGlu4/tyr, 1µM ATP, and 0.2µCi γ–ATP in addition to baculovirus-expressed GST-Met kinase. Reactions are halted by 8% TCA after an hour of incubation at 30 °C. A liquid scintillation counter is used to quantify the filters after TCA precipitates are gathered onto GF/C plates using a universal harvester.
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| Cell Assay |
The 96-well microtiter plates containing GTL-16 cells are seeded with 0.5% fetal calf serum. The plates are then incubated for 24 hours at 37°C, 5% CO2, 95% air, and 100% relative humidity before receiving a compound. A further 72 hours are spent treating cells with BMS-794833. Calculations are made for growth inhibition[1].
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| Animal Protocol |
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| References |
| Molecular Formula |
C23H15CLF2N4O3
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| Molecular Weight |
468.84
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| Exact Mass |
468.08
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| Elemental Analysis |
C, 58.92; H, 3.22; Cl, 7.56; F, 8.10; N, 11.95; O, 10.24
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| CAS # |
1174046-72-0
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| Related CAS # |
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| Appearance |
white solid powder
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| SMILES |
C1=CC(=CC=C1C2=CNC=C(C2=O)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F)F
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| InChi Key |
PDYXPCKITKHFOZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H15ClF2N4O3/c24-20-19(7-8-29-22(20)27)33-18-6-5-14(9-17(18)26)30-23(32)16-11-28-10-15(21(16)31)12-1-3-13(25)4-2-12/h1-11H,(H2,27,29)(H,28,31)(H,30,32)
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| Chemical Name |
N-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1H-pyridine-3-carboxamide
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| Synonyms |
BMS-794833; BMS 794833; BMS794833
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.33 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 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 (5.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1329 mL | 10.6646 mL | 21.3292 mL | |
| 5 mM | 0.4266 mL | 2.1329 mL | 4.2658 mL | |
| 10 mM | 0.2133 mL | 1.0665 mL | 2.1329 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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