Name | 2-[(6-Hydroxy-6-methyl-2-heptanyl)amino]-4-methyl-6-[(5-methyl-1H -pyrazol-3-yl)amino]nicotinonitrile hydrochloride (1:1) |
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Synonyms | TC-A 2317 hydrochloride |
Description | TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity[1]. |
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Related Catalog | |
Target |
Aurora A:1.2 nM (Ki) Aurora B:101 nM (Ki) |
In Vitro | TC-A 2317 hydrochloride (Compound 6) inhibits proliferation of HCT116 cells with an IC50 of 115 nM[1]. |
In Vivo | TC-A 2317 hydrochloride is effective in antitumor mice model without decrease of body weight[1]. TC-A 2317 hydrochloride shows good PK profile; Cmax value is 4930 nM (Tmax=1.2 h) and serum concentration after 24 h is 52 nM (T1/2=3.3 h) at 30 mg/kg po in rats[1]. Animal Model: HCT-116 Xenograft mice mode[1] Dosage: P.o.; daily for 14 days Administration: 30 mg/kg Result: Growth of tumor was inhibited by 59% after 14 days. |
References |
Molecular Formula | C19H29ClN6O |
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Molecular Weight | 392.92600 |
Exact Mass | 392.20900 |
PSA | 112.88000 |
LogP | 4.07528 |