A potent JNK inhibitor
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CC-930

Item No. 22466

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-4-[[9-[(3S)-tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]-cyclohexanol
CAS Number
899805-25-5
Synonyms
  • Tanzisertib
Molecular Formula
C21H23F3N6O2
Formula Weight
448.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH7.2)(1:20): 0.05 mg/ml
λmax
247, 336 nm
SMILES
O[C@@H]1CC[C@@H](NC2=NC(N([C@H]3CCOC3)C(NC4=C(F)C=C(F)C=C4F)=N5)=C5C=N2)CC1
InChi Code
InChI=1S/C21H23F3N6O2/c22-11-7-15(23)18(16(24)8-11)28-21-27-17-9-25-20(26-12-1-3-14(31)4-2-12)29-19(17)30(21)13-5-6-32-10-13/h7-9,12-14,31H,1-6,10H2,(H,27,28)(H,25,26,29)/t12-,13-,14-/m0/s1
InChi Key
IBGLGMOPHJQDJB-IHRRRGAJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $171

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    10 mg

    $302

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    25 mg

    $655

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    Product Description

    CC-930 is an orally bioavailable and potent inhibitor of JNKs (IC50s = 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively).1 It is selective for MAP kinases over a panel of 240 kinases, showing greater than 50% inhibition at only one non-MAP kinase target, EGFR (IC50 = 380 nM). Within the MAPK family, it is selective for JNKs having IC50 values of 3,400 and 480 nM for p38α and ERK1, respectively. CC-930 inhibits JNK in a cell lysate assay with an IC50 value of 200 nM and blocks the phosphorylation of c-Jun in stimulated human peripheral blood mononuclear cells (PBMCs). In rats, CC-930 (10 and 30 mg/kg) inhibits TNF-α production induced by LPS. It also reduces lung fibrosis in a dose-dependent manner in a mouse pulmonary fibrosis model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Krenitsky, V.P., Nadolny, L., Delgado, M., et al. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg. Med. Chem. Lett. 22(3), 1433-1438 (2012).