| Identification | Back Directory | [Name]
TC-A 2317 hydrochloride | [CAS]
1245907-03-2 | [Synonyms]
TC-A-2317 HCl
Reaxys ID: 20640556
TC-A 2317 hydrochloride
2-[(5-Hydroxy-1,5-dimethylhexyl)amino]-4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]-3-pyridinecarbonitrile hydrochloride
permeability,oral,Inhibitor,selective,antitumor,inhibit,HCT-116,TC A 2317 hydrochloride,TCA 2317 hydrochloride,Aurora Kinase,proliferation,TC-A 2317 | [Molecular Formula]
C19H29ClN6O | [MDL Number]
MFCD19690936 | [MOL File]
1245907-03-2.mol | [Molecular Weight]
392.93 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biochem/physiol Actions]
TC-A2317 (TC-A 2317) is an orally active, potent and selective aurora A kinase inhibitor (Ki = 1.2 nM; Aurora B Ki = 101 nM; IC50 >1 μM toward 60 other kinases). TC-A2317 inhibits the proliferation of human colorectal carcinoma HCT116 cells in cultures (IC50 = 115 nM) and suppresses HCT116 xenograft-derived tumor growth in mice in vivo (by 59% on day 14; 30 mg/kg/day p.o.) with good pharmacokinectic properties, oral bioavailability (Tmax = 1.2 h, T1/2 = 3.3 h, Cmax = 4930 nM, C60 min = 52 nM in rat serum post 30 mg/kg p.o.), and no adverse effects to the animals. TC-A231 is a racemate with its (S)-enantiomer being more active than the (R)-enantiomer (respective Ki = 0.59 vs. 66 nM). | [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.
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| [IC 50]
Aurora A: 1.2 nM (Ki); Aurora B: 101 nM (Ki) | [storage]
Store at +4°C | [References]
[1] Ando R, et al. 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. Bioorg Med Chem Lett. 2010;20(15):4709-4711. DOI:10.1016/j.bmcl.2010.04.119 |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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