343787-29-1

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
• CAS NO: 343787-29-1
• Molecular Formula: C24H27N5O2
• Molecular Weight: 417.50348
• Product Categories: Inhibitors
• Mol File: 343787-29-1.mol
• Article Data: 0

Chemical Properties

• Boiling Point: 656.3±65.0 °C(Predicted)
• Appearance: /
• Density: 1.32
• Solubility: insoluble in H2O; ≥2.39 mg/mL in EtOH with gentle warming and ultrasonic; ≥20.9 mg/mL in DMSO
• PKA: 9.84±0.20(Predicted)
• CAS DataBase Reference: 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine(CAS DataBase Reference)
• NIST Chemistry Reference: 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine(343787-29-1)
• EPA Substance Registry System: 1-{2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl}-piperidin-4-ylamine(343787-29-1)

Safety Data

• Hazardous Substances Data: 343787-29-1(Hazardous Substances Data)

Usage

Description

1-2-[5-(2-Methoxy-ethoxy)-benzoimidazol-1-yl]-quinolin-8-yl-piperidin-4-ylamine, also known as CP 673451, is a potent inhibitor of platelet-derived growth factor receptor β (PDGFR-β) with an IC50 of 1 nM. It is a complex organic compound characterized by its antiangiogenic and antitumor properties, making it a promising candidate for pharmaceutical applications.

Uses

1. Used in Pharmaceutical Applications:
CP 673451 is used as an inhibitor of PDGFR-β for its antiangiogenic and antitumor properties. It plays a crucial role in inhibiting the growth of new blood vessels that supply nutrients to the tumor, thereby limiting tumor growth and progression.
2. Used in Cancer Treatment:
CP 673451 is employed as a potent PDGFR-β inhibitor, particularly against various types of cancer. By targeting the PDGFR-β pathway, it can potentially disrupt the signaling mechanisms that promote cancer cell growth and survival.
3. Used in Drug Development:
CP 673451 serves as a valuable compound in the development of new drugs targeting PDGFR-β, which can be used in combination with other therapeutic agents to enhance the overall treatment efficacy against cancer.
4. Used in Research and Development:
CP 673451 is utilized in research and development for understanding the role of PDGFR-β in various diseases, including cancer, and for identifying potential synergistic effects when combined with other therapeutic agents.
5. Used in Drug Delivery Systems:
Similar to gallotannin, CP 673451 can also benefit from novel drug delivery systems to enhance its delivery, bioavailability, and therapeutic outcomes. These systems can help overcome limitations associated with the compound's solubility, stability, and targeted delivery to cancer cells.

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].

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.