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Tanzisertib(CC-930)

(Synonyms: JNK-930, JNKI-1) 目录号 : GC25982

Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.

Tanzisertib(CC-930) Chemical Structure

Cas No.:899805-25-5(freebase)

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5mg
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25mg
¥2,850.00
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Sample solution is provided at 25 µL, 10mM.

Description

Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.

CC-930 inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50 = 1 μM). CC-930 shows remarkable selectivity in a panel of 240 kinases, EGFR being the only non-MAP kinase inhibited more than 50% at 3 μM (IC50 = 0.38 μM). It inhibits no receptor at greater than 50% at 10 μM concentration in a panel of 75 receptors, ion channels and neurotransmitter transporters. CC-930 does not inhibit CYP P450 enzymes significantly and is metabolized by CYP 3A4 and 2D6[1].

In the acute rat LPS-induced TNFα production PK-PD model, the compound inhibits the production of TNFα by 23% and 77% at 10 and 30 mg/kg oral dose respectively. CC-930 is well-tolerated and exposure is dose-proportional[1].

[1] Plantevin Krenitsky V, et al. Bioorg Med Chem Lett. 2012, 22(3):1433-8.

化学性质

Cas No. 899805-25-5(freebase) SDF Download SDF
别名 JNK-930, JNKI-1
分子式 C21H23F3N6O2.HCl 分子量 484.9
溶解度 DMSO: 89 mg/mL (183.54 mM);Water: 4 mg/mL (8.25 mM);Ethanol: 89 mg/mL (183.54 mM) 储存条件 Store at -20°C
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1 mM 2.0623 mL 10.3114 mL 20.6228 mL
5 mM 0.4125 mL 2.0623 mL 4.1246 mL
10 mM 0.2062 mL 1.0311 mL 2.0623 mL
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