Tanzisertib(CC-930)

Catalog No.S8490 Synonyms: JNK-930, JNKI-1

For research use only.

Tanzisertib (CC-930, JNK-930, JNKI-1) 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.

Tanzisertib(CC-930) Chemical Structure

CAS No. 899805-25-5(freebase)

Selleck's Tanzisertib(CC-930) has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description Tanzisertib (CC-930, JNK-930, JNKI-1) 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.
Targets
JNK3 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
JNK1 [1]
(Cell-free assay)
0.006 μM 0.007 μM 0.061 μM
In vitro

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 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). It inhibits no receptor at greater than 50% at 10 μM concentration in a panel of 75 receptors, ion channels and neurotransmitter transporters. CC-930 does not inhibit CYP P450 enzymes significantly and is metabolized by CYP 3A4 and 2D6[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat T cells MnvHSpVv[3Srb36gZZN{[Xl? NV;tb2V{UW6qaXLpeIlwdiCxZjDKUmsudWWmaXH0[YQhT1OWIITh[4dm\CClLVr1ckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTpVzc2G2IGSgZ4VtdHNiY3;tdI92dmRidILlZZRm\CCob4KgN|AhdWmwczDwdolweiCjbnnzc416[2mwIIP0bY12dGG2aX;uJI1m[XO3cnXkJIFnfGW{IESwJI1qdnNiYomg[ox2d3Knc3PlcoNmKHOyZXP0do9xcG:2b33leJJ6NCCLQ{WwQVAvOiEQvF2= MoPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NES5N|coRjJ{MkS0PVM4RC:jPh?=
In vivo In 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[1].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: Jurkat T cells
  • Concentrations: --
  • Incubation Time: 30 minutes
  • Method: Jurkat T cells (5×105 /well) are aliquoted in 96 well membrane filter plates, then treated with or without compound 30 minutes prior to stimulation with 0.3 μg/ml anisomycin for an additional 40 minutes. Cells are pelleted under vacuum with plate manifold. Cell lysates are prepared by adding 75 μl/well lysis buffer (20 mM HEPES pH 7.4, 100 mM NaCl, 0.2% Triton X-100, 0.5 mM DTT, 2x phosphatase inhibitors, 20 mM PNPP, 1x protease inhibitors), for 30 minutes at room temperature. Lysates are filtered and collected into a new 96 well plate placed beneath the vacuum manifold. Cell lysates (45 μl) are added to an assay plate containing bound GST-c-Jun and MgCl2 in solution (10 mM) then incubated for 10 minutes at room temperature. The reaction is stopped by washing with Tris-buffered saline containing 0.02% Tween 20 and the phosphorylated GST-c-Jun detected by Europium labeled anti-phospho-c-Jun, DELFIA assay buffer and enhancement solution. Plate fluorescence is measured.
Animal Research:[1]
  • Animal Models: Male C57Bl/6 mice
  • Dosages: 2 mg/kg(i.v.) or 10 mg/kg(p.o.)
  • Administration: i.v. or p.o.

Solubility (25°C)

In vitro

DMSO 89 mg/mL warmed
(183.54 mM)
Ethanol 89 mg/mL warmed
(183.54 mM)
Water 4 mg/mL warmed
(8.24 mM)

Chemical Information

Molecular Weight 484.9
Formula

C21H23F3N6O2.HCl

CAS No. 899805-25-5(freebase)
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CCC1NC2=NC=C3C(=N2)N(C(=N3)NC4=C(C=C(C=C4F)F)F)C5CCOC5)O

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01466725 Terminated Drug: CC-930|Drug: Placebo Discoid Lupus Celgene November 1 2011 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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