Identification | Back Directory | [Name]
1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine | [CAS]
343787-29-1 | [Synonyms]
CS-464 CP 673451 CP 673451; CP673451 CP-673451;CP 673451;CP673451 1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine 1-[2-[5-(2-Methoxyethoxy)-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine 4-PiperidinaMine,1-[2-[5-(2-Methoxyethoxy)-1H-benziMidazol-1-yl]-8-quinolinyl]- 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine 1-(2-(5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl)quinolin-8-yl)piperidin-4-amine 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-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 USP/EP/BP 1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine CP 673451 | [Molecular Formula]
C24H27N5O2 | [MDL Number]
MFCD11100329 | [MOL File]
343787-29-1.mol | [Molecular Weight]
417.503 |
Chemical Properties | Back Directory | [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 | [pka]
9.84±0.20(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM. | [Definition]
ChEBI: 1-[2-[5-(2-methoxyethoxy)-1-benzimidazolyl]-8-quinolinyl]-4-piperidinamine is an aminoquinoline. | [Biological Activity]
cp-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]. | [target]
PDGFRβ | [storage]
Store 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. |
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