BMS-265246

製品コードS2014 バッチS201401

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₇F₂N₃O₂

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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. This compound 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. It exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent versus CDK1 and CDK2, respectively. This chemical represents the most potent CDK/CDK2 selective analogue from this chemotype. ^[1] A recent study shows that this compound inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of this chemical, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity. ^[2]

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.

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. This compound 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. It exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent versus CDK1 and CDK2, respectively. This chemical represents the most potent CDK/CDK2 selective analogue from this chemotype. ^[1] A recent study shows that this compound inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of this chemical, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	CDK1/Cyclin B1 Kinase Assay
キナーゼアッセイ	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 this compound.

参考

https://pubmed.ncbi.nlm.nih.gov/12824044/
https://pubmed.ncbi.nlm.nih.gov/21216932/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
WEE1 confers resistance to KRASG12C inhibitors in non-small cell lung cancer [ Cancer Lett, 2024, 611:217414]	PubMed: 39725152
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
Trapping KSHV in Latency-Exploring Kinase Inhibitors as a Class of Anti-Virals that Target the KSHV Lytic Cycle [ ProQuest, 2021, 28714138]	PubMed: None
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

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。

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