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Tanzisertib

Chemical Structure : Tanzisertib

CAS No.: 899805-25-5

Tanzisertib (CC-930, CC930)

Catalog No.: PC-27738Not For Human Use, Lab Use Only.

Tanzisertib (CC-930) is a potent, selective, ATP-competitive and orally active c-Jun N-terminal kinase (JNK) inhibitor with IC50 of 61/5/5 nM for JNK1/2/3 respectively.

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Biological Activity

Tanzisertib (CC-930) is a potent, selective, ATP-competitive and orally active c-Jun N-terminal kinase (JNK) inhibitor with IC50 of 61/5/5 nM for JNK1/2/3 respectively.
Tanzisertib (CC-930) is selective against MAP kinases ERK1 and p38α with IC50 of 0.48 and 3.4 μM respectively.
Tanzisertib (CC-930) has Ki values of 44 nM and 6.2 nM for JNK1 and JNK2 respectively.
Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 uM).
Tanzisertib (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).
Tanzisertib (CC-930) inhibited the production of TNFα by 23% and 77% at 10 and 30 mg/kg oral dose respectively in acute rat LPS-induced TNFα production PK-PD model.

Physicochemical Properties

M.Wt 448.45
Formula C21H23F3N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

trans-4-((9-((S)-tetrahydrofuran-3-yl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)cyclohexanol

References

1. Nagy MA, et al. J Med Chem. 2021 Dec 23;64(24):18193-18208.

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

3. Reich N, et al. Ann Rheum Dis. 2012 May;71(5):737-45.

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