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DB07268 Sale

(Synonyms: 2-[[2-[(3-羟基苯基)氨基]-4-嘧啶基]氨基]苯甲酰胺,DB 07268;DB-07268) 目录号 : GC14114

A potent inhibitor of JNK1

DB07268 Chemical Structure

Cas No.:929007-72-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,498.00
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5mg
¥1,350.00
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10mg
¥1,729.00
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50mg
¥4,043.00
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100mg
¥8,308.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

References:
[1] Liu M,Wang S,Clampit JE,Gum RJ,Haasch DL,Rondinone CM,Trevillyan JM,Abad-Zapatero C,Fry EH,Sham HL,Liu G.  Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. Bioorg Med Chem Lett.2007 Feb 1;17(3):668-72. Epub 2006 Nov 2.
[2] Romain Nol, Youseung Shin, Xinyi Song, Yuanjun He, Marcel Koenig, Weimin Chen, Yuan Yuan Ling, Li Lin, Claudia H.  Ruiz, Phil LoGrasso, Michael D. Cameron, Derek R. Duckett, Theodore M. Kamenecka. Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-Jun N-terminal kinase inhibitors.Bioorg Med Chem Lett. 2011 May 1; 21(9): 2732–2735.

Chemical Properties

Cas No. 929007-72-7 SDF
别名 2-[[2-[(3-羟基苯基)氨基]-4-嘧啶基]氨基]苯甲酰胺,DB 07268;DB-07268
化学名 2-[[2-(3-hydroxyanilino)pyrimidin-4-yl]amino]benzamide
Canonical SMILES C1=CC=C(C(=C1)C(=O)N)NC2=NC(=NC=C2)NC3=CC(=CC=C3)O
分子式 C17H15N5O2 分子量 321.33
溶解度 ≥ 15.2 mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.1121 mL 15.5603 mL 31.1207 mL
5 mM 0.6224 mL 3.1121 mL 6.2241 mL
10 mM 0.3112 mL 1.556 mL 3.1121 mL
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