Name:Tanzisertib(CC-930)
Synonyms:JNK-930, JNKI-1
CAS Number:899805-25-5(freebase)
Formula:C21H23F3N6O2.HCl
M.w.:484.9
DMSO (mg/mL)Max Solubility:89
DMSO (mM)Max Solubility:183.54
Form:hydrochloride
SMILES:Cl.OC1CCC(CC1)NC2=NC3=C(C=N2)N=C(NC4=C(F)C=C(F)C=C4F)[N]3C5CCOC5
ALogP:3.791
Target:JNK
Pathway:MAPK
Information: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.
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