2-(4-methylphenyl)-N-[4-(4-morpholinyl)phenyl]-4-quinazolinamine is a complex organic compound, also known as **Lapatinib**. It is a **tyrosine kinase inhibitor**, which means it blocks the activity of certain enzymes called tyrosine kinases.
**Why is Lapatinib important for research?**
Lapatinib is a clinically approved drug used in the treatment of **HER2-positive breast cancer**. This means it targets cancer cells that have an over-expression of the HER2 protein, a receptor that promotes cell growth.
**Here's how it works:**
* **Tyrosine kinases** are crucial for cell signaling pathways, controlling cell growth, division, and survival.
* **HER2** is one such tyrosine kinase that is often over-expressed in certain types of cancer, leading to uncontrolled cell proliferation.
* **Lapatinib** binds to and inhibits the activity of the HER2 protein, blocking its signaling pathways and ultimately hindering cancer cell growth.
**Beyond its clinical application, Lapatinib is important for research because:**
* **Target validation:** Its success in treating HER2-positive breast cancer validates HER2 as a crucial target for cancer therapy.
* **Drug development:** Lapatinib serves as a template for designing new and improved tyrosine kinase inhibitors, potentially for treating other cancers and diseases.
* **Understanding cancer biology:** Studies with Lapatinib help researchers understand the complex mechanisms of cancer development and how to effectively target specific pathways.
* **Combinatorial therapy:** Research explores combining Lapatinib with other therapies to enhance its efficacy and overcome resistance mechanisms.
**In summary, Lapatinib is a significant molecule due to its therapeutic value in treating HER2-positive breast cancer and its role in advancing research on targeted therapies, cancer biology, and drug development.**
ID Source | ID |
---|---|
PubMed CID | 1187531 |
CHEMBL ID | 1456553 |
CHEBI ID | 105138 |
Synonym |
---|
OPREA1_449277 |
OPREA1_673555 |
smr000429873 |
(4-morpholin-4-yl-phenyl)-(2-p-tolyl-quinazolin-4-yl)-amine |
MLS000767543 |
CHEBI:105138 |
2-(4-methylphenyl)-n-[4-(morpholin-4-yl)phenyl]quinazolin-4-amine |
STK840373 |
AKOS001664588 |
F3097-4376 |
n-(4-morpholinophenyl)-2-(p-tolyl)quinazolin-4-amine |
CHEMBL1456553 |
SR-01000499146-1 |
sr-01000499146 |
Q27182835 |
2-(4-methylphenyl)-n-[4-(4-morpholinyl)phenyl]-4-quinazolinamine |
2-(4-methylphenyl)-n-(4-morpholin-4-ylphenyl)quinazolin-4-amine |
Class | Description |
---|---|
morpholines | Any compound containing morpholine as part of its structure. |
[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, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 39.8107 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 23.9341 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 2.8184 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 23.0999 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
USP1 protein, partial | Homo sapiens (human) | Potency | 50.1187 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
TDP1 protein | Homo sapiens (human) | Potency | 19.7347 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 9.9150 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
Smad3 | Homo sapiens (human) | Potency | 22.3872 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 25.1189 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
67.9K protein | Vaccinia virus | Potency | 15.8489 | 0.0001 | 8.4406 | 100.0000 | AID720579 |
glucocerebrosidase | Homo sapiens (human) | Potency | 14.1254 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 31.6228 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
IDH1 | Homo sapiens (human) | Potency | 18.3564 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 35.4813 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 32.6427 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 15.8489 | 0.7943 | 21.2757 | 50.1187 | AID624246 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 11.2202 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 79.4328 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
geminin | Homo sapiens (human) | Potency | 10.3899 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0580 | 10.6949 | 26.6086 | AID602310 |
neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.5893 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
Glycoprotein hormones alpha chain | Homo sapiens (human) | Potency | 28.1838 | 4.4668 | 8.3448 | 10.0000 | AID624291 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
hormone activity | Glycoprotein hormones alpha chain | Homo sapiens (human) |
protein binding | Glycoprotein hormones alpha chain | Homo sapiens (human) |
follicle-stimulating hormone activity | Glycoprotein hormones alpha chain | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
extracellular region | Glycoprotein hormones alpha chain | Homo sapiens (human) |
extracellular space | Glycoprotein hormones alpha chain | Homo sapiens (human) |
Golgi lumen | Glycoprotein hormones alpha chain | Homo sapiens (human) |
follicle-stimulating hormone complex | Glycoprotein hormones alpha chain | Homo sapiens (human) |
pituitary gonadotropin complex | Glycoprotein hormones alpha chain | Homo sapiens (human) |
extracellular space | Glycoprotein hormones alpha chain | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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 | |||
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
[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] |