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Tanzisertib(CC-930)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tanzisertib(CC-930)图片
CAS NO:899805-25-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)448.44
FormulaC21H23F3N6O2
CAS No.899805-25-5 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol: N/A
SMILES CodeO[C@H]1CC[C@H](NC2=NC=C3N=C(NC4=C(F)C=C(F)C=C4F)N([C@@H]5COCC5)C3=N2)CC1
SynonymsCC930, JNK-930, JNKI-1, CC 930, Tanzisertib, JNK930, JNKI1, CC-930, JNK 930, JNKI 1
实验参考方法
In Vitro

In vitro activity: Tanzisertib (also known as CC-930) is a potent, specific and and orally bioavailable JNK1/JNK2/JNK3 inhibitor that has the potential to be used for the treatment of fibrotic and infammatory indications.Tanzisertib is in Phase 1 clinical trial and may have potential use for prevention and treatment of dermal fibrosis. 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 (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. CC-930 blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis.


Kinase Assay: CC-930 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.


Cell Assay: Systemic sclerosis (SSc) fibroblasts are incubated with 1 μM CC-930 in 96-well plates for 20 h. Then MTT is added at a final concentration of 1 mg/mL, and the cells are further incubated at 37°C for 4 h. Mock-treated fibroblasts are used as controls, and all other results are normalised to untreated cells.

In VivoIn 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.
Animal modelMale C57Bl/6 mice
Formulation & DosageDissolved in 5% DMA and 30% PEG 400 (i.v.) or 0.5% CMC/0.25% Tween80(p.o.); 2 mg/kg(i.v.) or 10 mg/kg(p.o.); i.v. or p.o.
ReferencesBioorg Med Chem Lett. 2012;22(3):1433-8; J Hepatol. 2014 Dec;61(6):1376-84; Ann Rheum Dis. 2012;71(5):737-45.
生物活性

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.