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| Product Name: | CC 930 | | Synonyms: | MCC930;CC 930;CC930;CC-930;trans-4-[[9-[(3S)-Tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]cyclohexanol;4-[[9-[(3s)-oxolan-3-yl]-8-(2,4,6-trifluoroanilino)purin-2-yl]amino]cyclohexan-1-ol;TANZISERTIB (CC-930);Tanzisertib(CC-930) (free base) | | CAS: | 899805-25-5 | | MF: | C21H23F3N6O2 | | MW: | 448.44 | | EINECS: | | | Product Categories: | MAPK | | Mol File: | 899805-25-5.mol |  |
| | CC 930 Chemical Properties |
| Boiling point | 626.4±65.0 °C(Predicted) | | density | 1.63±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder | | pka | 15.05±0.40(Predicted) | | color | Off-white to yellow |
| | CC 930 Usage And Synthesis |
| Uses | Tanzisertib is a potent, selective, and orally active c-Jun amino-terminal kinase (JNK) inhibitor used for treatment of dermal fibrosis. | | Biological Activity | Tanzisertib (CC-930, JNK-930, JNKI-1) has an ATP-competitive inhibitory effect on the phosphorylation of the JNK-dependent protein substrate c-Jun and 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), selective inhibition of ERK1 and p38a with IC50 of 0.48 μM and 3.4 μM, respectively . | | in vivo | In the acute PK-PD rat model of LPS-induced TNFα production, oral administration of 10 mg/kg and 30 mg/kg of CC-930 reduced the production of TNFα in vivo by 23% and 77%, respectively. CC-930 is well tolerated in vivo and its effect is proportional to dose. | | target | | Target | Value | JNK3
(Cell-free assay) | 0.006 μM | JNK2
(Cell-free assay) | 0.007 μM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> JNK1
(Cell-free assay) 0.061 μM |
| | IC 50 | JNK3: 6 nM (IC50); JNK2: 7 nM (IC50); JNK1: 61 nM (IC50) |
| | CC 930 Preparation Products And Raw materials |
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