1-(4-methoxyphenyl)-N-[2-(4-morpholinyl)ethyl]-4-pyrazolo[3,4-d]pyrimidinamine is a chemical compound often referred to as **Pazopanib**.
**Pazopanib** is a **tyrosine kinase inhibitor**, which means it blocks the activity of certain enzymes called tyrosine kinases. These enzymes play a crucial role in cell signaling and growth. Pazopanib specifically targets several tyrosine kinases, including:
* **VEGFRs (Vascular Endothelial Growth Factor Receptors):** These receptors are involved in the formation of new blood vessels (angiogenesis), a process crucial for tumor growth.
* **PDGFRs (Platelet-Derived Growth Factor Receptors):** These receptors are involved in cell proliferation and survival, which can contribute to tumor growth.
* **c-KIT:** This receptor is involved in cell development and proliferation, and it is often overexpressed in certain cancers.
**Why Pazopanib is Important for Research:**
Pazopanib is important for research due to its potential therapeutic applications in various areas:
* **Cancer Treatment:** Pazopanib has been approved by the FDA for treating **renal cell carcinoma (RCC)** and **soft tissue sarcomas**. It works by inhibiting the growth of cancer cells by blocking the signaling pathways that promote their proliferation and survival.
* **Other Potential Applications:** Pazopanib is being studied in clinical trials for other types of cancer, including **breast cancer, colorectal cancer, and lung cancer**. It is also being investigated for its potential use in treating **rheumatoid arthritis, inflammatory bowel disease, and diabetic retinopathy**.
* **Understanding of Tyrosine Kinase Inhibition:** The study of Pazopanib and other tyrosine kinase inhibitors has contributed significantly to our understanding of how these enzymes function and how their inhibition can be therapeutically beneficial. This knowledge is crucial for the development of new and more effective therapies for a range of diseases.
**Overall, Pazopanib is a significant molecule in the field of cancer research and therapy. Its effectiveness in treating certain cancers and its potential for other therapeutic applications make it an important subject of ongoing research.**
ID Source | ID |
---|---|
PubMed CID | 1985423 |
CHEMBL ID | 1472430 |
CHEBI ID | 107981 |
Synonym |
---|
MLS000556538 |
[1-(4-methoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-4-yl]-(2-morpholin-4-yl-ethyl)-amine |
smr000147855 |
OPREA1_318047 |
CHEBI:107981 |
1-(4-methoxyphenyl)-n-(2-morpholin-4-ylethyl)pyrazolo[3,4-d]pyrimidin-4-amine |
HMS2357F12 |
AKOS022118018 |
CHEMBL1472430 |
1-(4-methoxyphenyl)-n-[2-(morpholin-4-yl)ethyl]-1h-pyrazolo[3,4-d]pyrimidin-4-amine |
STL336444 |
1-(4-methoxyphenyl)-n-[2-(4-morpholinyl)ethyl]-4-pyrazolo[3,4-d]pyrimidinamine |
Q27186336 |
SR-01000566503-1 |
sr-01000566503 |
Class | Description |
---|---|
ring assembly | Two or more cyclic systems (single rings or fused systems) which are directly joined to each other by double or single bonds are named ring assemblies when the number of such direct ring junctions is one less than the number of cyclic systems involved. |
pyrazoles | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 28.1838 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 39.8107 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 15.1014 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 12.4518 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 14.1254 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 79.4328 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 20.5962 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 5.6234 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.56) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |