CCT 137690

Research use only, not for human use.

A potent, orally bioavailable Aurora kinases inhibitor with IC50 of 15/25/19 nM for Aurora A/B/C; displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI50=0.30 uM) and A2780 ovarian cancer cell line (GI50=0.14 uM).

A potent, orally bioavailable Aurora kinases inhibitor with IC50 of 15/25/19 nM for Aurora A/B/C; displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI50=0.30 uM) and A2780 ovarian cancer cell line (GI50=0.14 uM); exhibits in vivo efficacy with no observed toxicities in SW620 colon carcinoma xenografts.

CCT 137690 displays antiproliferative activity in a range of human tumor cell lines, including SW620 colon carcinoma (GI50=0.30 μM) and A2780 ovarian cancer cell line (GI50=0.14 μM). CCT 137690 inhibits in vitro phosphorylation of histone H3. CCT 137690 is a moderate inhibitor of the hERG ion-channel (IC50=3.0 μM). CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis.

CCT 137690 slows the growth of the SW620 xenografts with no observed toxicity. CCT 137690 significantly inhibits tumour growth in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation.

CCT-137690 | CCT137690

Cell Cycle/DNA Damage

Aurora Kinase

AuroraA|AuroraB|AuroraC

Cancer

——

1095382-05-0

551.4813

C26H31BrN8O

>98% (HPLC)

10 mM in DMSO

CN1CCN(C2=CC=C(C3=NC4=C(N5CCN(CC6=NOC(C)=C6)CC5)C(Br)=CN=C4N3)C=C2)CC1

3H-Imidazo[4,5-b]pyridine, 6-bromo-7-[4-[(5-methyl-3-isoxazolyl)methyl]-1-piperazinyl]-2-[4-(4-methyl-1-piperazinyl)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years