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IRAK inhibitor 1 Sale

(Synonyms: 环巴胺抑制剂1) 目录号 : GC17158

An IRAK4 inhibitor

IRAK inhibitor 1 Chemical Structure

Cas No.:1042224-63-4

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5mg
¥1,838.00
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10mg
¥2,510.00
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50mg
¥6,069.00
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500mg
¥31,080.00
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1g
¥48,615.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

IC50: 35 nM for IRAK-4

The interleukin-1 receptor associated kinase (IRAK) family is comprised of four family members IRAK-1, IRAK-2, IRAK-3/M, and IRAK-4. Upon activation of their upstream cognate receptors, IRAK-4 is thought to phosphorylate IRAK-1 resulting in the activation and autophosphorylation of IRAK-1 an subsequent phosphorylation of downstream substrates. IRAK inhibitor 1 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4).

In vitro: The regioisomeric pyridines IRAK inhibitor 1 (6) and it analogue (7) showed contrasting SAR, with the 2,6-pyridine isomer IRAK inhibitor 1 having low-nanomolar potency whilst the 2,4-pyridine isomer 7 showed little activity, despite having a more accessible bidentate-binding motif. At 10 μM, IRAK inhibitor 1 was found to have 39% inhibition for JNK-1 and 15% inhibition for JNK-2, respectivley [1].

In vivo: No animal in-vivo data available currently IRAK inhibitor 1 and its analogues.

Clinical trial: IRAK inhibitor 1 is currently in the preclinical development stage and no clinical data are available.

Reference:
[1] Buckley GM, Ceska TA, Fraser JL, Gowers L, Groom CR, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V.   IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008;18(11):3291-5.

Chemical Properties

Cas No. 1042224-63-4 SDF
别名 环巴胺抑制剂1
化学名 6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine
Canonical SMILES C1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4
分子式 C17H19N5 分子量 293.37
溶解度 DMSO : 16.67 mg/mL (56.82 mM; Need ultrasonic) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.4087 mL 17.0433 mL 34.0866 mL
5 mM 0.6817 mL 3.4087 mL 6.8173 mL
10 mM 0.3409 mL 1.7043 mL 3.4087 mL
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