| Identification | Back Directory | [Name]
CC 930 | [CAS]
899805-25-5 | [Synonyms]
CC930
CC-930
MCC930
CC 930
CS-1152
Tanzisertib
CC-930(Tanzisertib)
TANZISERTIB (CC-930)
TANZISERTIB; CC930; CC 930
Tanzisertib(CC-930) (free base)
4-[[9-[(3s)-oxolan-3-yl]-8-(2,4,6-trifluoroanilino)purin-2-yl]amino]cyclohexan-1-ol
trans-4-[[9-[(3S)-Tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]cyclohexanol
Cyclohexanol, 4-[[9-[(3S)-tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]-, trans- | [Molecular Formula]
C21H23F3N6O2 | [MDL Number]
MFCD23160040 | [MOL File]
899805-25-5.mol | [Molecular Weight]
448.44 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C |
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