BMS-794833 1174046-72-0
Product Description
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Biological Activity
BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM.
In GTL-16 human gastric tumor xenografts model, BMS798433 shows greater
than 50% TGI for at least one tumor doubling time with no overt toxicity
observed during 14 days. BMS798433 also shows complete tumor stasis at a
dose of 25 mg/kg against U87 glioblastoma model.
Met kinase assay
BMS798433 is dissolved in DMSO and diluted by water before use. The
reaction solution contains baculovirus expressed GST-Met kinase, 20 mM
Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 0.1 mg polyGlu4/tyr,
1µM ATP and 0.2µCi γ–ATP. Reactions are incubated at 30 °C for 1 hour
and stopped by 8% TCA. TCA precipitates are collected onto GF/C plates
using a universal harvester and the filters are quantitated using liquid
scintillation counter.
VEGFR2 assay
BMS798433
is dissolved in DMSO and diluted by water before use. The reaction
solution contains 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 75 µg polyGlu4/tyr, 1µM ATP, 0.5 µCi γ–ATP and 7.5 ng/rxn enzyme stock (10% glyc
Method
GTL-16 cells are seeded into 96 well plates and incubated for 24 hours.
BMS798433 is dissolved in DMSO at 10 mM and diluted with culture medium
before use. Then BMS798433 is added to the cells for 72 hours. After
that, MTS assay is used to measure the IC50.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Chemical Information
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Contact us if you need more details on 1174046-72-0. We are ready to answer your questions on packaging, logistics, certification or any other aspects about BMS-794833 1174046-72-0、1174046-72-0 BMS-794833. If these products fail to match your need, please contact us and we would like to provide relevant information.
Biological Activity
BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM.
In GTL-16 human gastric tumor xenografts model, BMS798433 shows greater
than 50% TGI for at least one tumor doubling time with no overt toxicity
observed during 14 days. BMS798433 also shows complete tumor stasis at a
dose of 25 mg/kg against U87 glioblastoma model.
Met kinase assay
BMS798433 is dissolved in DMSO and diluted by water before use. The
reaction solution contains baculovirus expressed GST-Met kinase, 20 mM
Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 0.1 mg polyGlu4/tyr,
1µM ATP and 0.2µCi γ–ATP. Reactions are incubated at 30 °C for 1 hour
and stopped by 8% TCA. TCA precipitates are collected onto GF/C plates
using a universal harvester and the filters are quantitated using liquid
scintillation counter.
VEGFR2 assay
BMS798433
is dissolved in DMSO and diluted by water before use. The reaction
solution contains 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 75 µg polyGlu4/tyr, 1µM ATP, 0.5 µCi γ–ATP and 7.5 ng/rxn enzyme stock (10% glyc
Method
GTL-16 cells are seeded into 96 well plates and incubated for 24 hours.
BMS798433 is dissolved in DMSO at 10 mM and diluted with culture medium
before use. Then BMS798433 is added to the cells for 72 hours. After
that, MTS assay is used to measure the IC50.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 468.84 |
---|---|
Formula | C23H15ClF2N4O3 |
CAS No. | 1174046-72-0 |
Storage | 3 years -20℃Powder |
---|---|
6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | |
Solubility (25°C) * | In vitro | DMSO | 94 mg/mL (200.49 mM) |
---|---|---|---|
Water | <1 mg/mL ( | ||
Ethanol | <1 mg/mL ( | ||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name | N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on 1174046-72-0. We are ready to answer your questions on packaging, logistics, certification or any other aspects about BMS-794833 1174046-72-0、1174046-72-0 BMS-794833. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : Protein Tyrosine Kinase > c-Met Inhibitor
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