產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 50mg
CAS	1808011-22-4
別名	N/A
化學(xué)名	6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluorobutyl)piperidin-4-yl)methyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
分子式	C26H34ClF3N4O4S
分子量	591.09
溶解度	Soluble in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

IC50: 3 nM

EPZ031686 is the first SMYD3 inhibitor.

Set and Mynd Domain containing 3 (SMYD3), a lysine methyltransferase (KMT) expressed at high levels in a number of different cancer histologies, is reported to be associated with a poor clinical prognosis.

In vitro: EPZ031686 was the first SMYD3 inhibitor found to show double-digit nanomolar cellular activity. In addition, EPZ031686 displayed noncompetitive inhibition to both SAM and MEKK2 with a Ki = 1.2 and 1.1 nM, respectively. Moreover, EPZ031686 showed less than 30% inhibition against 16 histone methyltransferase targets at a 10 μM [1].

In vivo: Male mice i.v. administered a single dose of EPZ031686 at 1 mg/kg showed a moderate clearance of 27 mL/min/kg, which was in very good agreement with the microsomal data, with a volume of distribution at steady state of 2.3 L/kg, translating to a terminal half-life of 1.7 h. Around 20% of the administered dose was excreted unchanged in urine after 24 h, equivalent to a renal clearance of 5.3 mL/min/kg. Bioavailability of 48 and 69 was observed at 5 and 50 mg/kg, respectively, resulting in the EPZ031686 unbound blood concentration remaining above the SMYD3 IC50 value for more than 12 h after a 50 mg/kg p.o. administration [1].

Clinical trial: Up to now, EPZ031686 is still in the preclinical development stage.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項：

1.遵守中華人民共和國有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請您真實的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個人或團體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細地址*
常用郵箱*
請輸入您對我們的意見或建議*
驗證碼*