| 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 | [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). | [storage]
Store at +4°C |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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