Tanzisertib

SKU: orb1308483

Description

Tanzisertib (CC-930) is a potent and selective JNK1/2/3 inhibitor with respective IC50 values of 61, 7, and 6 nM. It has demonstrated antifibrotic activity in preclinical research, showing efficacy in both in vitro assays and in vivo models of fibrotic diseases.

Research Area

Signal Transduction

Key Properties

• CAS Number: 899805-25-5
• MW: 448.44
• Purity: 99.28%
• Formula: C₂₁H₂₃F₃N₆O₂
• SMILES: N(C=1N(C=2C(N1)=CN=C(N[C@H]3CC[C@H](O)CC3)N2)[C@H]4CCOC4)C5=C(F)C=C(F)C=C5F
• Target: JNK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.46 mM);DMSO:33 mg/mL (73.59 mM)

Bioactivity

• Target IC50:
  JNK1:61 nM|JNK3:6 nM|JNK2:7 nM
• In Vivo:
  Tanzisertib (CC-930), when administered orally at doses of 10 and 30 mg/kg, decreases TNFa production by 23% and 77% respectively in the acute rat LPS-induced TNFa production PK-PD model. Additionally, at a dose of 150 mg/kg, Tanzisertib (CC-930) not only prevents the development of fibrosis across various models but also reverses 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) and blocks the JNK pathway activated by pro-fibrotic cytokines in systemic sclerosis. Tanzisertib (CC-930) (1-2 μM) substantially reduces and abrogates apoptosis and necrosis in hepatocytes, including FC-loaded WT hepatocytes.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CC 930, CC930, CC-930, inhibit, JNK3, JNK1, JNK2, JNK, Inhibitor, Tanzisertib

Compound Identifiers

PubChem CID

11597537