3H-IMidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)Methyl]-1-piperazinyl]-2-(1,3-diMethyl-1H-pyrazol-4-yl)-
3H-IMidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)Methyl]-1-piperazinyl]-2-(1,3-diMethyl-1H-pyrazol-4-yl)- Basic information
- Product Name:
- 3H-IMidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)Methyl]-1-piperazinyl]-2-(1,3-diMethyl-1H-pyrazol-4-yl)-
- Synonyms:
-
- 3H-IMidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)Methyl]-1-piperazinyl]-2-(1,3-diMethyl-1H-pyrazol-4-yl)-
- 6-chloro-7-[4-[(4-chlorophenyl)methyl]piperazin-1-yl]-2-(1,3-dimethylpyrazol-4-yl)-1H-imidazo[4,5-b]pyridine
- CCT241736
- CCT241736;CCT-241736;CCT 241736
- CS-2683
- 6-Chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyridine
- CCT 241736,Fms like tyrosine kinase 3,CCT241736,CD135,Inhibitor,FLT3,CCT-241736,Aurora Kinase,Cluster of differentiation antigen 135,inhibit
- 1-[6-chloro-2-(1,3-dimethyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyridin-7-yl]-4-[(4-chlorophenyl)methyl]piperazine
- CAS:
- 1402709-93-6
- MF:
- C22H23Cl2N7
- MW:
- 456.37
- Product Categories:
-
- API
- Mol File:
- 1402709-93-6.mol
3H-IMidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)Methyl]-1-piperazinyl]-2-(1,3-diMethyl-1H-pyrazol-4-yl)- Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:75.0(Max Conc. mg/mL);164.34(Max Conc. mM)
- form
- A crystalline solid
- color
- White to off-white
3H-IMidazo[4,5-b]pyridine, 6-chloro-7-[4-[(4-chlorophenyl)Methyl]-1-piperazinyl]-2-(1,3-diMethyl-1H-pyrazol-4-yl)- Usage And Synthesis
Uses
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
in vivo
CCT241736 (50, 100 mg/kg, b.i.d, p.o.) dose-dependently suppresses the growth of MV4-11 human tumor xenografts, and completely abolishes the tumors at 100 mg/kg via p.o. administration twice a day[1].
IC 50
Aurora-A: 38 nM (IC50); Aurora-A: 7.5 nM (Kd); Aurora-B: 48 nM (Kd); FLT3(K663Q): 5.1 nM (Kd); FLT3: 6.2 nM (Kd); FLT3(D835H): 11 nM (Kd); FLT3(D835Y): 14 nM (Kd); FLT3(N841I): 16 nM (Kd); FLT3-ITD: 38 nM (Kd); FLT3(R834Q): 110 nM (Kd)
References
[1] Bavetsias V, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem. 2012 Oct 25;55(20):8721-34. DOI:10.1021/jm300952s
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