BMS-357075
BMS-357075 is a pan-CDK inhibitor with CDK1 IC50 18 nM, CDK2 IC50 3 nM, CDK4 IC50 26 nM. BMS-357075 induces cytotoxicity in human ovarian cancer A2780 cells. BMS-357075 exhibits anticancer activity in mice against P388 murine leukemia. BMS-357075 can be used for the research of leukemia.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 350509-99-8
- 分子式: C22H31N5O2S2
- 分子量:461.64
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
CDK1/cyclinB1 18 nM (IC50) |
CDK2/cyclinE 3 nM (IC50) |
CDK4/cyclin D 26 nM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
3 nM
Compound: 19
|
Cytotoxic effect on human ovarian (A2780) cancer cell line
Cytotoxic effect on human ovarian (A2780) cancer cell line
|
[PMID: 15125971] |
体外実験
BMS-357075 (compound 19) potently inhibits CDK1/cyclin B (IC50 = 18 nM), CDK2/cyclin E (IC50 = 3 nM), and CDK4/cyclin D (IC50 = 26 nM) in cell-free enzyme assays[1].
BMS-357075 potently inhibits the viability of human ovarian cancer A2780 cells with an IC50 of 3 nM[1].
BMS-357075 shows 90% protein binding in mouse serum[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 350509-99-8
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分子量 461.64
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分子式 C22H31N5O2S2
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SMILES
OCC(C)(CNCC1=CN=C(NC2=NC=C(SCC3=NC=C(C(C)(C)C)O3)S2)C=C1)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)