Patupilone (Epothilone B)

製品コードS1364 バッチS136403

化学情報

	Synonyms	EPO906	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₇H₄₁NO₆S
	分子量	507.68	CAS No.	152044-54-7
Solubility (25°C)*	体外	DMSO	102 mg/mL (200.91 mM)
		Ethanol	102 mg/mL (200.91 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	Patupilone (EPO906, Epothilone B) is a paclitaxel-like microtubule-stabilizing agent with EC_0.01 of 1.8 μM. Phase 2.
in vitro	Epothilone B shows better activity than Epothilone A. The EC_0.01 of Epothilone B is 1.8 μM. Epothilone B potently inhibits cell proliferation in HCT116 cells, with IC50 of 0.8 nM. ^[1] Epothilone B induces mitotic arrest and displays cytotoxicity in KB3-1, KBV-1, Hela, and Hs578T cells, with IC50 of 3 nM to 92 nM. Epothilone B competes with Taxol in binding to microtubules, with IC50 of 3.3 μM. ^[2] In MCF-7 cells overexpressing GFP-α-tubulin, Epothilone B (3.5 nM) efficiently blocks microtubule dynamics. Meanwhile, Epothilone B induces mitotic arrest with IC50 of 3.5 nM. ^[3] In multiple myeloma (MM) cells, including RPMI 8226, U266, MM.1S, LR5, and MR20, Epothilone B directly suppresses proliferation with IC50 of 1 nM to 10 nM. Similarly, Epothilone B (10 nM) also induces cell cycle arrest and apoptosis. ^[4] A recent study reveals that, in ovarian cancer Hey cells, Epothilone B (5 nM–100 nM) enhances surface epithelial cell adhesion antigen (EpCAM), without affecting the transcription or the total cellular level of EpCAM. ^[5]
in vivo	In a mouse xenograft model of RPMI 8226 cells, Epothilone B (2.5 mg/kg–4 mg/kg) prolongs survival and suppresses tumor growth. ^[4] Similarly, in mouse xenograft models of prostate cancer cells, including DU145 and PC3, Epothilone B at the same dose also inhibits tumor growth. ^[6]

プロトコル(参考用のみ)

キナーゼアッセイ	Tubulin polymerization assay
キナーゼアッセイ	Calf brain microtubule proteins (MTP) are purified, which includes approximately 15%–20% microtubule associated proteins. The buffer (MES buffer) used for the Epothilone B-microtubule studies contains 0.1 M 2-morpholinoethanesulfonic acid (MES), 1 mM EGTA, 0.5 mM MgCl₂, and 3 M glycerol at pH 6.6. Samples for electron microscopy are placed on carbon-over-Parlodion-coated grids (300 mesh) and negatively stained with 2% uranyl acetate. Microtubule assembly in the presence or absence of Epothilone B is monitored spectrophotometrically by using a spectrophotometer equipped with a thermostatically regulated liquid circulator. The temperature is held at 35 °C and changes in turbidity (representative of polymer mass) are monitored at 350 nm. Effective concentration (EC_0.01), defined as the interpolated concentration capable of inducing an initial slope of 0.01 OD/min rate, is calculated using the formula EC_0.01 = concentration/slope and expressed as the mean with standard deviation obtained from three different concentrations.
細胞アッセイ	細胞株	KB3-1, KBV-1, Hela, and Hs578T cells
	濃度	0–1 μM
	反応時間	72 hours
	実験の流れ	For mitotic block and aberrant mitosis, cells are plated either in 48-well plates (for trypan blue and cell counting) or onto coverslips. After 24 hours, cells are treated with Epothilone B and scored at regular intervals. For the cytotoxicity analysis, cells are counted and scored as trypan blue positive or negative. Concurrently, coverslips andaliquots of cells in the culture supernatant are fixed and stained with Hoechst33342 in PBS. These cells are scored for cells blocked at the G2/M transition and aberrant mitosis.
動物実験	動物モデル	Mice xenograft model of RPMI 8226 cells
	投薬量	2.5 mg/kg–4 mg/kg
	投与方法	Inject intravenously

参考

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カスタマーフィードバック

: , , Oncotarget, 2015, 6(13):10893-907.

: , , J Cancer Res Clin Oncol, 2016, 142(11):2281-9.

: Data independently produced by , , Dr. Helen Sadik of Johns Hopkins University

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：

Rehabilitation enhances epothilone-induced locomotor recovery after spinal cord injury [ Brain Commun, 2023, 5(1):fcad005]	PubMed: 36744011
A new form of axonal pathology in a spinal model of neuromyelitis optica [ Brain, 2022, awac079]	PubMed: 35202467
Tubulin isotypes optimize distinct spindle positioning mechanisms during yeast mitosis [ J Cell Biol, 2021, 220(12)e202010155]	PubMed: 34739032
Various effects of two types of kinesin-5 inhibitors on mitosis and cell proliferation [ Biochem Pharmacol, 2021, 193:114789]	PubMed: 34582773
Epothilones Improve Axonal Growth and Motor Outcomes after Stroke in the Adult Mammalian CNS [ Cell Rep Med, 2020, 1(9):100159]	PubMed: 33377130
Deletion of Glutathione S-Transferase Omega 1 Activates Type I Interferon Genes and Downregulates Tissue Factor [ Cancer Res, 2020, canres.530.2020]	PubMed: 32571799
Paclitaxel Enhances the Innate Immunity by Promoting NLRP3 Inflammasome Activation in Macrophages. [ Front Immunol, 2019, 10:72]	PubMed: 30761140
CETSA-based target engagement of taxanes as biomarkers for efficacy and resistance [ Sci Rep, 2019, 9(1):19384]	PubMed: 31852908
Systemic administration of epothilone D improves functional recovery of walking after rat spinal cord contusion injury [Ruschel J, et al. Exp Neurol, 2018, 306:243-249]	PubMed: 29223322
Epothilone B impairs functional recovery after spinal cord injury by increasing secretion of macrophage colony-stimulating factor [ Cell Death Dis, 2017, 8(11):e3162]	PubMed: 29095439

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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