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((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamic acid 2,6-bis(1-methylethyl)phenyl ester

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamic acid 2,6-bis(1-methylethyl)phenyl ester, also known as **bosutinib**, is a small molecule tyrosine kinase inhibitor (TKI). It's important for research due to its potential therapeutic applications, particularly in the treatment of **cancer**.

Here's a breakdown:

* **Tyrosine kinase inhibitors (TKIs):** These are drugs that block the activity of specific tyrosine kinases, enzymes that play a crucial role in cell signaling pathways. Abnormal tyrosine kinase activity can contribute to the development and progression of various diseases, including cancer.
* **Bosutinib's Target:** Bosutinib primarily targets the **ABL** and **KIT** tyrosine kinases, which are often overactive in certain types of cancer.
* **Clinical Applications:** Bosutinib has been approved by the FDA for the treatment of:
* **Chronic myeloid leukemia (CML)**: A type of blood cancer where the ABL gene is fused to another gene, resulting in the production of an abnormal tyrosine kinase.
* **Ph+ acute lymphoblastic leukemia (ALL)**: A type of childhood leukemia where the ABL gene is also fused to another gene.
* **GIST (Gastrointestinal Stromal Tumor)**: A rare type of cancer that originates in the gastrointestinal tract and involves the KIT tyrosine kinase.

**Research Importance:**

* **Novel Treatment Options:** Bosutinib provides a valuable therapeutic option for patients with these specific types of cancers, often improving their survival and quality of life.
* **Understanding Cancer Biology:** The research into bosutinib and its effects on various tyrosine kinases contributes to a deeper understanding of the mechanisms driving cancer development and progression.
* **Development of New Therapies:** Research on bosutinib can lead to the development of new and improved TKIs with better efficacy, fewer side effects, and broader applicability.

**Note:** Bosutinib is a prescription drug and should only be used under the supervision of a qualified healthcare professional.

Let me know if you have any other questions!

((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamic acid 2,6-bis(1-methylethyl)phenyl ester: a water soluble inhibitor of ACAT; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3025787
CHEMBL ID22279
SCHEMBL ID13765697
MeSH IDM0228543

Synonyms (20)

Synonym
2,6-bis(1-methylethyl)phenyl[[2,6-bis(1-methylethyl)phenoxy]sulfonyl]carbamate
bdbm50050318
((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamic acid 2,6-bis(1-methylethyl)phenyl ester
CHEMBL22279 ,
[2,6-di(propan-2-yl)phenyl] n-[2,6-di(propan-2-yl)phenoxy]sulfonylcarbamate
pd138142-15
2,6-bis(1-methylethyl)phenyl ((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamate
bis(2,6-mepo)-cns
carbamic acid, ((2,6-bis(1-methylethyl)phenoxy)sulfonyl)-, 2,6-bis(1-methylethyl)phenyl ester
pd138142 ,
pd-138142-15
pd-138142
pd 138142
142642-31-7
carbamic acid,[[2,6-bis(1-methylethyl)phenoxy]sulfonyl]-, 2,6-bis(1-methylethyl)phenyl ester(9ci)
SCHEMBL13765697
ci-999
DTXSID20162114
AKOS030610835
2,6-diisopropylphenyl (2,6-diisopropylphenoxy)carbonylsulfamate
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID21182Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 4 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID174746Acute in vivo activity measured by total plasma cholesterol concentration levels (TC) at 30 mg/kg dose1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID21169Solution Degradation Studies measured by compound unchanged at pH 0.4=50% 1 M HCl/50% acetonitrile at 0 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID21179Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 0 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID21173Solution Degradation Studies measured by compound unchanged at pH 0.4=50% 1 M HCl/50% acetonitrile at 8 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID21180Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 2 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID21181Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 24 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID21172Solution Degradation Studies measured by compound unchanged at pH 0.4=50% 1 M HCl/50% acetonitrile at 4 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID31668In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase 1 in microsomes of rat liver1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID174734Chronic in vivo activity was measured by the concentration of high density lipoproteins (HDL) in cholesterol fed rats1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID21170Solution Degradation Studies measured by compound unchanged at pH 0.4=50% 1 M HCl/50% acetonitrile at 2 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID174747Acute in vivo activity was measured by the total plasma cholesterol concentration levels(TC) at dose 3 mg/kg1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID21171Solution Degradation Studies measured by compound unchanged at pH 0.4=50% 1 M HCl/50% acetonitrile at 24 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID174751Chronic in vivo activity was measured by the total cholesterol concentration levels in cholesterol fed rats1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID21183Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 8 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's6 (85.71)18.2507
2000's1 (14.29)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.10

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.

MetricThis Compound (vs All)
Research Demand Index12.10 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]