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Epothilone D

Epothilone D

产品编号 TQ0202   CAS 189453-10-9
别名: KOS 862, 埃博霉素

Epothilone D (KOS 862) is an effective microtubule stabilizer.

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Epothilone D Chemical Structure
Epothilone D, CAS 189453-10-9
规格 价格/CNY 货期 数量
2 mg ¥ 1,100 5日内发货
5 mg ¥ 1,860 5日内发货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Epothilone D (TQ0202)
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参考文献
结构类型
产品描述 Epothilone D (KOS 862) is an effective microtubule stabilizer.
体外活性 Epothilone D is a more potent microtubule stabilizer in vitro than epothilone A or B. In vitro, Epothilone D has shown potent cytotoxicity in a panel of human tumor cell lines, with similar potency to paclitaxel. Epothilone D also shows a definite advantage over paclitaxel in drug-resistant cell lines and retained its cytotoxicity against a multidrug-resistant cell line over-expressing P-glycoprotein [1].
体内活性 To evaluate whether Epothilone D improves MT and axonal function in PS19 mice, groups of 3-month old male PS19 mice received weekly i.p. injections of vehicle or Epothilone D (1 mg/kg or 3 mg/kg) for a total of 3 months. In addition, 3-month old non-Tg littermates received 3 mg/kg Epothilone D or vehicle. The 3 mg/kg Epothilone D dose corresponds to ~10-fold less than that used in Phase II clinical study, which should minimize side-effects such as neutropenia that are observed with MT-stabilizing drugs in human subjects. PS19 and WT mice that receive Epothilone D show no signs of drug intolerance. Indeed, all drug-treated mice exhibited weight gain that is indistinguishable from vehicle-treated animals. Likewise, relative organ weights are similar in vehicle- and Epothilone D-treated mice. The motor performance of Epothilone D-treated mice, assessed using a standard rotarod test, is not significantly different from vehicle-treated cohorts [2].
动物实验 Groups of mice (n=3) receive intraperitoneal (i.p.) injections of 3.7 mg/kg of Epothilone D (epoD) dissolved in 100% DMSO, followed by euthanization using approved at times ranging from 0.25 h to 24 h. In another study, groups of mice (n=3) receive injections of 3 mg/kg of epoD in 100% DMSO followed by euthanization 4, 6 and 10 days later. The Epothilone D (epoD) levels in the brain and blood samples are determined using LC-MS/MS protocols. Groups (n=10-13) of 3-month old PS19 tau Tg mice or 3-month old non-Tg littermates are administered weekly i.p. injections of 1 mg/kg epoD, 3 mg/kg of Epothilone D (epoD) or vehicle (DMSO), for a total of 3 months. Animals are monitored for signs of abnormal behavior or distress and are weighed weekly. After final dosing, the mice undergo motor function and cognitive testing. After euthanization, brains and optic nerve (ON) are recovered for immunohistochemical analyses. A subset of mice from each group also undergo necropsy evaluation with organ weights recorded [2].
别名 KOS 862, 埃博霉素
分子量 491.68
分子式 C27H41NO5S
CAS No. 189453-10-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 300 mg/mL (610.15 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0338 mL 10.1692 mL 20.3384 mL 50.8461 mL
5 mM 0.4068 mL 2.0338 mL 4.0677 mL 10.1692 mL
10 mM 0.2034 mL 1.0169 mL 2.0338 mL 5.0846 mL
20 mM 0.1017 mL 0.5085 mL 1.0169 mL 2.5423 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0169 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL

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TargetMol Library Books参考文献

1. Konner J, et al. Phase I clinical, pharmacokinetic, and pharmacodynamic study of KOS-862 (Epothilone D) in patients with advanced solid tumors and lymphoma. Invest New Drugs. 2012 Dec;30(6):2294-302. 2. Brunden KR, et al. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J Neurosci. 2010 Oct 13;30(41):13861-6.
MAP4343 Tubulin inhibitor 7 Dolastatin 10 Terflavoxate Sovilnesib MT189 Maytansine ARN25068

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Keywords

Epothilone D 189453-10-9 Cytoskeletal Signaling Microtubule Associated KOS-862 KOS862 KOS 862 埃博霉素 Inhibitor inhibitor inhibit

 

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