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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.

Images & Validation

Key Properties

CAS Number1095382-05-0
MW551.4813
Purity>98% (HPLC)
FormulaC26H31BrN8O
SMILESCN1CCN(C2=CC=C(C3=NC4=C(N5CCN(CC6=NOC(C)=C6)CC5)C(Br)=CN=C4N3)C=C2)CC1
TargetAurora Kinase
Solubility10 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.
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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CCT-137690 | CCT137690

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  • CCT 137690 [orb1305267]

    >99.99% (May vary between batches)

    1095382-05-0

    551.48

    C26H31BrN8O

    5 mg, 10 mg, 25 mg, 50 mg, 1 ml x 10 mM (in DMSO), 1 mg
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Protocol Information

CCT 137690 (orb1226996)

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Available Sizes

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200 mg
500 mg
2 mg
¥ 1,300.00
5 mg
¥ 1,690.00
10 mg
¥ 1,950.00
25 mg
¥ 3,380.00
50 mg
¥ 5,850.00
100 mg
¥ 8,840.00