1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine

1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine Basic information
Product Name:1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
Synonyms:1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine;CP 673451;1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine;4-PiperidinaMine,1-[2-[5-(2-Methoxyethoxy)-1H-benziMidazol-1-yl]-8-quinolinyl]-;1-(2-(5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine;1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine CP 673451;1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine CP 673451;CP-673451;CP 673451;CP673451
CAS:343787-29-1
MF:C24H27N5O2
MW:417.5
EINECS:
Product Categories:Inhibitors
Mol File:343787-29-1.mol
1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine Structure
1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine Chemical Properties
Boiling point 656.3±65.0 °C(Predicted)
density 1.32
storage temp. Store at -20°C
solubility insoluble in H2O; ≥2.39 mg/mL in EtOH with gentle warming and ultrasonic; ≥20.9 mg/mL in DMSO
form Powder
pka9.84±0.20(Predicted)
Safety Information
MSDS Information
1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine Usage And Synthesis
UsesCP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.
Uses1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine exhibits antiangiogenic and antitumor properties. It is an inhibitor of platelet-derived growth factor receptor β (PDGFR- β).
DefinitionChEBI: 1-[2-[5-(2-methoxyethoxy)-1-benzimidazolyl]-8-quinolinyl]-4-piperidinamine is an aminoquinoline.
Biological Activitycp-673451 is a potent inhibitor of pdgfr with ic50 value of 10nm and 1nm for pdgfr-α and pdgfr-β, respectively [1].cp-673451 is an atp-competitive inhibitor and is investigated to treat for cancer. it is highly selective against pdgfr-α and pdgfr-β over a variety of other kinases such as vegfr-1, vegfr-2, lck, tie-2 and egfr. in pae-β cells, cp-673451 inhibits pdgfr-β with ic50 value of 6.4nm. cp-673451 also inhibits c-kit with ic50 value of 1.1μm in h526 cells. in rat c6 glioblastoma xenograft models, a single oral dose of 50mg/kg cp-673451 reduces > 50% phosphorylation of pdgfr-β for 4 hours. in addition, cp-673451 is found to inhibit pdgf-bb-induced angiogenesis in a sponge angiogenesis model. furthermore, cp-673451 inhibits the tumor growth in colo205, ls174t, h460, and u87mg xenograft models. it also reduces the microvessel density of colo205 xenografts [1].
targetPDGFRβ
storageStore at -20°C
references[1] roberts w g, whalen p m, soderstrom e, et al. antiangiogenic and antitumor activity of a selective pdgfr tyrosine kinase inhibitor, cp-673,451. cancer research, 2005, 65(3): 957-966.
1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine Preparation Products And Raw materials
Crenolanib (CP-868596) Sunitinib Malate NVP-BGJ398 2-Methoxyethoxymethyl chloride MK-2206 2HCl CYCLOPAMINE Y27632 (hydrochloride) 2-MERCAPTO-5-METHOXYBENZIMIDAZOLE

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