BMS-794833 化学構造
分子量: 468.84




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  • 研究分野



製品説明 BMS794833は、MetとVEGFR2の強力なATP競争的阻害剤で、IC50 がそれぞれ 1.7 nM と 15 nMです。
ターゲット Met VEGFR2
IC50 1.7 nM 15 nM [1]
In vitro試験 BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM. [1]
In vivo試験 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. [1]
臨床試験 BMS798433 is currently in Phase I clinical trial against advanced or metastatic solid tumor.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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

細胞アッセイ: [1]

細胞株 GTL-16 cells
濃度 ~ 1 μM
反応時間 72 hours
実験の流れ 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.

動物実験: [1]

動物モデル GTL-16 and U87 xenografts
投薬量 25 mg/kg
投与方法 Orally once daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
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)



Download BMS-794833 SDF
分子量 468.84


CAS No. 1174046-72-0
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (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.
化学名 N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID