1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
Synonym(s):1-[2-[5-(2-Methoxyethoxy)-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine;1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine;
- CAS NO.:343787-29-1
- Empirical Formula: C24H27N5O2
- Molecular Weight: 417.5
- MDL number: MFCD11100329
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 18:09:03
What is 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine?
The Uses of 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.
The Uses of 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
1-[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).
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].
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.
Properties of 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
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 |
Safety information for 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine
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