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規格	10mM (in 1mL DMSO) 5mg 10mg 50mg 100mg
CAS	929007-72-7
別名	DB 07268;DB-07268
化學名	2-[[2-(3-hydroxyanilino)pyrimidin-4-yl]amino]benzamide
分子式	C17H15N5O2
分子量	321.33
溶解度	≥ 15.2 mg/mL 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

產品描述：

IC50: 9 nM for JNK1

DB07268 is a JNK1 inhibitor. The c-Jun N-terminal kinases (JNKs) are members of the mitogen-activated protein kinase family. Three JNK isoforms (JNK1, 2 and 3) have been identified. There is growing evidences indicating that activation of the JNK activity is involved in a number of human disease settings. Therefore, considerable efforts have been directed toward the identification of JNK inhibitors suitable for clinical development.

In vitro: The selectivity data of DB07268 against a panel of kinases has been tested. Results showed that DB07268 had some degree of selectivity over quite a few kinases with the exceptions of PLK, CHK1, and CK2. Although d DB07268 showed submicromolar potency against these three kinases, it still appeared to exhibit at least 70- to 90-fold greater potency against JNK1 than PLK, CHK1, and CK2 [1].

In vivo: Several analogs of DB07268 were profiled in vivo. These compounds had a range of exposure in rats and mice. Some had excellent brain penetration despite having poor rat pharmacokinetics, while others had a more balanced profile. Unfortunately, the most potent analog exhibited poor rat pk demonstrated by a short half-life, low oral absorption and poor brain penetration. One DB07268 analog likely exhibited modest rat pk with low clearance and decent oral absorption. This analog also showed modest brain penetration [1].

Clinical trial: So far, no clinical study has been reported.

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1. 本產品僅供科研使用。請勿用于醫藥、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。

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原創作者：上海莼試生物技術有限公司

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DB07268

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