2-(1,3-Benzothiazol-2-yl)-4-chloro-5-(3-chloroanilino)-3-pyridazinone, also known as **Bosutinib**, is an **important drug** used in the treatment of **chronic myeloid leukemia (CML)** and **Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL)**.
Here's why it's important for research:
* **Mechanism of Action:** Bosutinib is a **tyrosine kinase inhibitor (TKI)**. It specifically targets and inhibits the activity of **BCR-ABL**, a fusion protein that is the main driver of CML and Ph+ ALL. BCR-ABL is a constitutively active tyrosine kinase that promotes uncontrolled cell proliferation and survival. Bosutinib prevents BCR-ABL from functioning, thereby stopping the growth of leukemia cells.
* **Clinical Significance:** Bosutinib has been shown to be **effective in treating both newly diagnosed and resistant CML patients**, as well as those with Ph+ ALL. It has a good safety profile and a high response rate, making it a valuable treatment option.
* **Ongoing Research:** Continued research on Bosutinib focuses on:
* **Improving its efficacy and safety:** Researchers are investigating optimal dosing strategies, combinations with other therapies, and potential side effects.
* **Understanding its mechanism of action:** Studying how Bosutinib interacts with BCR-ABL and other cellular targets can lead to the development of even more effective treatments.
* **Exploring its potential in other cancers:** Bosutinib may be effective in treating other cancers that involve BCR-ABL or other tyrosine kinases.
**In summary, Bosutinib is a crucial drug for the treatment of CML and Ph+ ALL. Its effectiveness, safety profile, and ongoing research efforts contribute to its importance in medical research and patient care.**
ID Source | ID |
---|---|
PubMed CID | 6618919 |
CHEMBL ID | 1594333 |
CHEBI ID | 105144 |
Synonym |
---|
MLS000583096 , |
2-(1,3-benzothiazol-2-yl)-4-chloro-5-[(3-chlorophenyl)amino]pyridazin-3(2h)-one |
smr000206282 |
CHEMDIV2_003039 |
CHEBI:105144 |
HMS1377K03 |
2-(1,3-benzothiazol-2-yl)-4-chloro-5-[(3-chlorophenyl)amino]-2,3-dihydropyridazin-3-one |
AKOS001786633 |
2-(1,3-benzothiazol-2-yl)-4-chloro-5-(3-chloroanilino)pyridazin-3-one |
HMS2541J08 |
CCG-129077 |
CHEMBL1594333 |
Q27182842 |
2-(1,3-benzothiazol-2-yl)-4-chloro-5-(3-chloroanilino)-3-pyridazinone |
Class | Description |
---|---|
benzothiazoles | |
[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 | 7.9433 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 4.7755 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 70.7946 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
BRCA1 | Homo sapiens (human) | Potency | 14.1254 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 2.5929 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 11.5821 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 13.1205 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 50.1187 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
P53 | Homo sapiens (human) | Potency | 2.8184 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 3.9811 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 1.6360 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 71.1260 | 5.8048 | 36.1306 | 65.1308 | AID540253; AID540263 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 3.9811 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
snurportin-1 | Homo sapiens (human) | Potency | 71.1260 | 5.8048 | 36.1306 | 65.1308 | AID540253; AID540263 |
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 95.2834 | 0.4256 | 12.0591 | 28.1838 | AID504891 |
GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 16.3601 | 5.8048 | 16.9962 | 25.9290 | AID540253 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 22.3872 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 0.1995 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 10.0000 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID651635 | Viability Counterscreen for 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. |
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. |
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] |