CCT137690 1095382-05-0

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Molecular Weight:

551.48 CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.


Biological Activity


CCT137690
displays antiproliferative activity in a range of human tumor cell
lines, including SW620 colon carcinoma cell and A2780 ovarian cancer
cell with GI50 of 0.3 and o.14 μM, respectively. In addition, CCT137690
also inhibit the phosphorylation of histone H3. CCT137690 inhibits the
major cytochrome P450 isoforms (CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6,
CYP3A4) with IC50 greater than 10 μM. However, CCT137690 is a moderate
inhibitor of the hERG ion-channel with IC50 of 3.0 μM.


CCT137690 effectively inhibits the growth of human tumor cell lines of
different origins with GI50 ranging from 0.005 to 0.47 μM. CCT137690
completely inhibits both Aurora A autophosphorylation at T288 and
histone H3 phosphorylation at 0.5 μM. CCT137690 induces polyploidy,
mitotic aberrations, and Apoptosis in HCT116 cells. CCT137690 reduces
MYCN levels and GSK3β phosphorylation in the KELLY neuroblastoma cell
line. CCT137690 inhibits autophosphorylation of FLT3 and phosphorylation of its downstream targets STAT5 and p44/42 MAPK (Erk1/2).


CCT137690 is highly orally bioavailable and inhibits the growth of SW620
colon carcinoma xenografts with no observed toxicities as defined by
body weight loss. CCT137690 inhibits growth of MYCN-induced neuroblastoma at a dose of 100 mg/kg. Additionally, CCT137690 achieves target modulation and potently
inhibits the growth of subcutaneous MOLM-13 xenografts, with no obvious
toxicity or loss of body weight.

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Product Categories : Epigenetics > Aurora Kinase Inhibitor