CCT 137690

SKU: orb1226996

Description

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.

Key Properties

• CAS Number: 1095382-05-0
• MW: 551.4813
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₁BrN₈O
• SMILES: CN1CCN(C2=CC=C(C3=NC4=C(N5CCN(CC6=NOC(C)=C6)CC5)C(Br)=CN=C4N3)C=C2)CC1
• Target: Aurora Kinase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.
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• In Vitro:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CCT-137690 | CCT137690

Quick Database Links

Gene Symbol

Aurora Kinase