Tanzisertib(CC-930)

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

Tanzisertib(CC-930) Chemical Structure

Molecular Weight(MW): 484.9

CC-930 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.

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Biological Activity

Description CC-930 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 Mn6zSpVv[3Srb36gZZN{[Xl? NVXPcIp4UW6qaXLpeIlwdiCxZjDKUmsudWWmaXH0[YQhT1OWIITh[4dm\CClLVr1ckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTpVzc2G2IGSgZ4VtdHNiY3;tdI92dmRidILlZZRm\CCob4KgN|AhdWmwczDwdolweiCjbnnzc416[2mwIIP0bY12dGG2aX;uJI1m[XO3cnXkJIFnfGW{IESwJI1qdnNiYomg[ox2d3Knc3PlcoNmKHOyZXP0do9xcG:2b33leJJ6NCCLQ{WwQVAvOiEQvF2= NYrs[mZ{OjJ{NES5N|c>

... Click to View More Cell Line Experimental Data

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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Male C57Bl/6 mice
  • Formulation: 5% DMA and 30% PEG 400 (i.v.) or 0.5% CMC/0.25% Tween80(p.o.)
  • Dosages: 2 mg/kg(i.v.) or 10 mg/kg(p.o.)
  • Administration: i.v. or p.o.
    (Only for Reference)

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)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 484.9
Formula

C21H23F3N6O2.HCl

CAS No. 899805-25-5 (free base)
Storage powder
in solvent
Synonyms JNK-930|JNKI-1

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01466725 Terminated Discoid Lupus Celgene Corporation November 2011 Phase 2
NCT01203943 Terminated Idiopathic Pulmonary Fibrosis|Pulmonary Fibrosis|Fibrosis|Interstitial Lung Disease|Lung Diseases Interstitial Celgene Corporation|Celgene January 2011 Phase 2

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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.

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JNK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID