Purvalanol A

製品コードS7793 バッチS779301

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	C₁₉H₂₅ClN₆O
	分子量	388.89	CAS No.	212844-53-6
Solubility (25°C)*	体外	DMSO	60 mg/mL warmed with 50ºC water bath (154.28 mM)
		Ethanol	13 mg/mL warmed with 50ºC water bath (33.42 mM)
		Water	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
in vitro	Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells.^[2] Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells. ^[3]

製品説明

Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.

in vitro

Purvalanol A decreases cell viability in dose-dependent manner in MCF-7 and MDA-MB-231 cell lines. Purvalanol A induces cell viability loss by 50 % in MCF-7 cells but MDA-MB-231 cells sre less sensitive to Purvalanol A (32 % decreases in cell viability). Purvalanol A induces mitochondria-mediated apoptosis in MCF-7 and MDA-MB-231 cells.^[2] Purvalanol A effectively prevents c-Src-mediated transformation by inhibiting both cell cycle progression and c-Src signaling, and effectively suppresses the anchorage independent growth of some human cancer cells in which c-Src is up-regulated. Purvalanol A has a stronger inhibitory effect on the anchorage-independent growth of HT29 and SW480 human colon cancer cells. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MCF-7 and MDA-MB 231 breast cancer cells
	濃度	100 μM
	反応時間	24 h
	実験の流れ	Cells are seeded at 10000 density in 96-well plates and treated with various concentrations of Purvalanol A (0-100 μM) for 24 h. Cells are exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltet- razolium bromide dye (5 mg/mL) and are incubated at 37℃ for 4 h. In order to solubilize the formazan crystals 100 μL DMSO is added. Absorbance is determined at 570 nm spectrophotometrically.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Cancer Lett, 2016, 383(2):295-308]

: Data from [Data independently produced by , , J Biol Chem, 2016, 291(28):14761-72.]

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：

ASPP2 Is Phosphorylated by CDK1 during Mitosis and Required for Pancreatic Cancer Cell Proliferation [ Cancers (Basel), 2023, 10.3390/cancers15225424]	PubMed: 38001686
Combined inactivation of CTPS1 and ATR is synthetically lethal to MYC-overexpressing cancer cells [ Cancer Res, 2022, canres.1707.2021]	PubMed: 35022212
MARK2 regulates chemotherapeutic responses through class IIa HDAC-YAP axis in pancreatic cancer [ Oncogene, 2022, 41(31):3859-3875]	PubMed: 35780183
Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer [ Breast Cancer Res, 2022, 24(1):41]	PubMed: 35715861
The phosphatase CTDSPL2 is phosphorylated in mitosis and a target for restraining tumor growth and motility in pancreatic cancer [ Cancer Lett, 2021, 526:53-65]	PubMed: 34813892
Phosphorylation of CRMP2 by Cdk5 Negatively Regulates the Surface Delivery and Synaptic Function of AMPA Receptors [ Mol Neurobiol, 2021, 10.1007/s12035-021-02581-w]	PubMed: 34773219
Target RNA modification for epigenetic drug repositioning in neuroblastoma: computational omics proximity between repurposing drug and disease [ Aging (Albany NY), 2020, 12(19):19022-19044]	PubMed: 33044945
Transcriptome Analysis and Functional Identification of Adipose-Derived Mesenchymal Stem Cells in Secondary Lymphedema [ Gland Surg, 2020, 9(2):558-574]	PubMed: 32420291
LIMD1 phosphorylation in mitosis is required for mitotic progression and its tumor-suppressing activity. [ FEBS J, 2019, 286(5):963-974]	PubMed: 30600590
The Toxmatrix: Chemo-Genomic Profiling Identifies Interactions That Reveal Mechanisms of Toxicity [ Chem Res Toxicol, 2018, 31(2):127-136]	PubMed: 29156121

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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