Tanzisertib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tanzisertib (CC-930) 是一种有效的 JNK1/2/3 抑制剂，IC50 分别为 61/7/6 nM，具有潜在的抗纤维化活性。 Tanzisertib (CC-930) 抑制人 PBMC 刺激中磷酸化 cJun 的形成由 phorbol-12-myristate-13-acetate 和植物血凝素 (IC50=1 μM)[1] 组成，它阻断系统性硬化症中促纤维化细胞因子激活的 JNK 通路。

Tanzisertib (CC-930) is a potent inhibitor of JNK1/2/3 with IC50s of 61/7/6 nM, respectively, with potential antifibrotic activity.Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM) and it blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis. Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes.Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models. However, it can also induce the regression of pre-existing fibrosis.(In Vitro):Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM). Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. Tanzisertib (CC-930) blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis.(In Vivo):Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis.

Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM). Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. Tanzisertib (CC-930) blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis.

Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis.

CC-930

MAPK/ERK Signaling

JNK

JNK3|JNK2|JNK1

Respiratory system

Idiopathic Pulmonary Fibrosis; Pulmonary Fibrosis; Fibrosis; Interstitial Lung Disease; Lung Diseases, Interstitial

899805-25-5

448.44

C21H23F3N6O2

>98% (HPLC)

DMSO:33 mg/mL (73.59 mM)

O[C@H]1CC[C@@H](CC1)NC2=NC=C3N=C(N(C3=N2)[C@@H]4COCC4)NC5=C(C=C(C=C5F)F)F

——

(-20℃)

With Ice Pack

≥ 2 years