CC-930 is a potent, selective, and orally active JNK inhibitor with potential antifibrotic activity. CC-930 entered Phase I clinical trials. Tanzisertib may have potential use for prevention and treatment of dermal fibrosis. Selective inhibition of JNK by CC-930 exerted potent antifibrotic effects in vitro and in different models in vivo. JNK might thus be a novel molecular target for the treatment of fibrosis in SSc.
Chemical Formula: C21H23F3N6O2
Exact Mass: 448.18346
Molecular Weight: 448.44
Elemental Analysis: C, 56.24; H, 5.17; F, 12.71; N, 18.74; O, 7.14
(1S,4r)-4-((9-((S)-tetrahydrofuran-3-yl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)cyclohexanol JNK-930; JNKI-1
Appearance: White to off-white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
Gan LT, Van Rooyen DM, Koina M, McCuskey RS, Teoh NC, Farrell GC. Hepatocyte free cholesterol lipotoxicity results from JNK1-mediated mitochondrial injury and is HMGB1 and TLR4-dependent. J Hepatol. 2014 Jul 23. pii: S0168-8278(14)00523-6. doi: 10.1016/j.jhep.2014.07.024. [Epub ahead of print] PubMed PMID: 25064435.
Atsriku C, Hoffmann M, Ye Y, Kumar G, Surapaneni S. Metabolism and disposition of a potent and selective JNK inhibitor [14C]tanzisertib following oral administration to rats, dogs and humans. Xenobiotica. 2015 May;45(5):428-41. doi: 10.3109/00498254.2014.990949. PubMed PMID: 25482583.
Atsriku C, Hoffmann M, Moghaddam M, Kumar G, Surapaneni S. In vitro metabolism of a novel JNK inhibitor tanzisertib: interspecies differences in oxido-reduction and characterization of enzymes involved in metabolism. Xenobiotica. 2015;45(6):465-80. doi: 10.3109/00498254.2014.991367. PubMed PMID: 25475995.
Products are for research use only. Not for human use.
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