BMS-265246 化学構造
分子量: 345.34

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Quality Control & MSDS

製品説明

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製品の説明

生物活性

製品説明 BMS-265246は、CDK1/cycBとCDK2/cycEのための強力で選択的なCDK1/CDK2阻害剤で、IC50 がそれぞれ 6 nM と 9 nMです。
ターゲット CDK1/cyclin B CDK2/cyclin E
IC50 6 nM 9 nM [1]
In vitro試験 BMS265246 inhibits the activity of CDK4/cycD with IC50 of 0.23 μM and prevents A2780 Cytox with IC50 of 0.76 μM. BMS265246 which binds to CDK2 shows the inhibitor resides coincident with the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone. BMS265246 exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent versus CDK1 and CDK2, respectively. BMS265246 represents the most potent CDK/CDK2 selective analogue from this chemotype. [1] A recent study shows that BMS-265246 inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of BMS-265246, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity. [2]
In vivo試験
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

CDK1/Cyclin B1 Kinase Assay Kinase reactions consists of 100 ng of baculovirus expressed GST-CDK1/cyclin B1 complex, 1 μg histone H1, 0.2 μCi 33P γ-ATP, 25 μM ATP in 50 μL of kinase buffer (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT). Reactions are incubated for 45 min at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration of 15%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester, and the filters are quantitated using a TopCount 96 well liquid scintillation counter. Dose response curves are generated to determine the concentration required to inhibit 50% of kinase activity (IC50). BMS265246 is dissolved at 10 mM in DMSO and evaluated at six concentrations, each in triplicate. The final concentration of DMSO in the assay equals 2%. IC50 values are derived by nonlinear regression analysis and have a coefficient of variance (SD/mean, n = 6) = 16%.
CDK2/Cyclin E Kinase Assay Kinase reactions consists of 5 ng of baculovirus expressed GST-CDK2/cyclin E complex, 0.5 μg GST-RB fusion protein (amino acids 776−928 of retinoblastoma protein), 0.2 μCi 33P γ-ATP, and 25 μM ATP in 50 μL of kinase buffer (50 mM HEPES, pH 8.0, 10 mM MgCl

細胞アッセイ: [2]

細胞株 HCT116
濃度 0-5 μM
反応時間 24 hours
実験の流れ HCT-116 cells are plated onto 96-well dishes. For each well, the cell density is calculated by counting the number of objects (cells) per field of view, and averaging across all fields for a given well. For a treatment compound, cell density is converted to a percentage relative to the plate-averaged cell density from DMSO treatment (i.e., 100% corresponds to the average cell density for DMSO treatment). Logistic regression curve fits are done using TIBCO Spotfire, and the concentration at which the curve crosses 50% is reported as the EC50 of BMS-265246.

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
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)
1

参考

化学情報

Download BMS-265246 SDF
分子量 345.34
化学式

C18H17F2N3O2

CAS No. 582315-72-8
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 20 mg/mL (57.91 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 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 (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)methanone

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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