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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H17F2N3O2 |
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分子量 | 345.34 | CAS No. | 582315-72-8 | |
Solubility (25°C)* | 体外 | DMSO | 20 mg/mL (57.91 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4. |
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in vitro | 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] |
キナーゼアッセイ | CDK1/Cyclin B1 Kinase Assay | |
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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%. | ||
細胞アッセイ | 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. |
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CDC7 inhibition induces replication stress-mediated aneuploid cells with an inflammatory phenotype sensitizing tumors to immune checkpoint blockade [ Nat Commun, 2023, 10.1038/s41467-023-43274-3] | PubMed: 37980406 |
Nascent transcriptome reveals orchestration of zygotic genome activation in early embryogenesis [ Curr Biol, 2022, 32(19):4314-4324.e7] | PubMed: 36007528 |
Non-catalytic allostery in α-TAT1 by a phospho-switch drives dynamic microtubule acetylation [ J Cell Biol, 2022, 221-11e202202100] | PubMed: 36222836 |
Olaparib Induced Senescence is Bypassed through G2/M Checkpoint Override in Olaparib Resistant Prostate Cancer [ Mol Cancer Ther, 2022, molcanther.0604.2021] | PubMed: 35086956 |
Bromodomain-Containing Protein BRD4 Is Hyperphosphorylated in Mitosis [ Cancers (Basel), 2020, 12(6):E1637] | PubMed: 32575711 |
Inducing and exploiting vulnerabilities for the treatment of liver cancer [ Nature, 2019, 10.1038/s41586-019-1607-3] | PubMed: 31578521 |
Inducing and exploiting vulnerabilities for the treatment of liver cancer. [ Nature, 2019, 574(7777):268-272] | PubMed: 31578521 |
The TRAPP complex mediates secretion arrest induced by stress granule assembly. [ EMBO J, 2019, 38(19):e101704] | PubMed: 31429971 |
CDK9 modulates circadian clock by attenuating REV-ERBα activity. [ Biochem Biophys Res Commun, 2019, 513(4):967-973] | PubMed: 31005255 |
Nuclear Nestin deficiency drives tumor senescence via lamin A/C-dependent nuclear deformation. [ Nat Commun, 2018, 9(1):3613] | PubMed: 30190500 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。