Tag: M.W=100-150

Authors Thorve, PR; Maji, B in ROYAL SOC CHEMISTRY published article about in [Thorve, Pradip Ramdas; Maji, Biplab] Indian Inst Sci Educ & Res Kolkata, Dept Chem Sci, Mohanpur 741246, India in 2021, Cited 72. Recommanded Product: 88-68-6. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Herein, we report a bioinspired catalytic system for the one-pot cascade oxidation of a native primary amine and an in situ generated non-native secondary amine. The catalyst consists of an o-quinone cofactor phd (1,10-phenanthroline-5,6-dione) and a copper ion and operates under ambient air conditions. Quinazolin-4(3H)-ones, which are common pharmacophores present in numerous pharmaceuticals and bioactive compounds, were synthesized in high yields. A detailed kinetic and mechanistic study elucidates the role of the catalyst in the multi-step oxidative cascade reaction.

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Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

In 2019.0 MOL CANCER THER published article about ACQUIRED-RESISTANCE; CAPRI-GOIM; PLUS CETUXIMAB; INHIBITOR; MUTATIONS in [Martini, Giulia; Cardone, Claudia; Vitiello, Pietro Paolo; Belli, Valentina; Napolitano, Stefania; Troiani, Teresa; Ciardiello, Davide; Della Corte, Carminia Maria; Morgillo, Floriana; Matrone, Nunzia; Ciardiello, Fortunato; Martinelli, Erika] Univ Campania L Vanvitelli, Med Oncol, Dept Precis Med, Via Pansini 5, I-80131 Naples, Italy; [Sforza, Vincenzo] Fdn Pascale, IRCCS, Ist Nazl Tumori, Dept Clin Expt Thorac Oncol, Naples, Italy; [Papaccio, Gianpaolo; Desiderio, Vincenzo; Tirino, Virginia] Univ Campania Luigi Vanvitelli Napoli, Dept Expt Med, Naples, Italy; [Paul, Mariel C.; Moreno-Viedma, Veronica; Sibilia, Maria] Med Univ Vienna, Comprehens Canc Ctr, Dept Med 1, Inst Canc Res, Borschkegasse 8a, Vienna, Austria; [Normanno, Nicola; Rachiglio, Anna Maria] Fdn Pascale, IRCCS, Ist Nazl Tumori, Cell Biol & Biotherapy Unit, Naples, Italy; [Maiello, Evaristo; Latiano, Tiziana Pia; Rizzi, Daniele] Hosp Casa Sollievo Della Sofferenza San Giovanni, Med Oncol, San Giovanni Rotondo, Italy; [Signoriello, Giuseppe] Univ Campania L Vanvitelli, Biostat, Dipartimento Salute Mentale & Fis & Med Prevent, Naples, Italy in 2019.0, Cited 24.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8. Safety of 1-Phenylurea

The EPHA2 tyrosine kinase receptor is implicated in tumor progression and targeted therapies resistance. We evaluated EPHA2 as a potential resistance marker to the antiepidermal growth factor receptor (EGFR) monoclonal antibody cetuximab in colorectal cancer. We studied activation of EPHA2 in a panel of human colorectal cancer cell lines sensitive or resistant to anti-EGFR drugs. The in vitro and in vivo effects of ALW-II-41-27 (an EPHA2 inhibitor) and/or cetuximab treatment were tested. Fonnalin-fixed paraffin-embedded tumor specimens from 82 RAS wild-type (WV) metastatic colorectal cancer patients treated with FOLFIRI + cetuximab as first-line therapy in the CAPRI-COIM trial were assessed for EPHA2 expression by immunohistochemistry and correlated with treatment efficacy. EPHA2 was differentially activated in colorectal cancer cell lines. Combined treatment with ALW-II-41-27 plus cetuximab reverted primary and acquired resistance to cetuximab, causing cell growth inhibition, inducing apoptosis and cell-cycle G1-G2 arrest. In tumor xenograft models, upon progression to cetuximab, ALW-II-41-27 addition significantly inhibited tumor growth. EPHA2 protein expression was detected in 55 of 82 tumor samples, frequently expressed in less-differentiated and left-sided tumors. High levels of EPHA2 significantly correlated with worse progression-free survival [8.6 months; confidence interval (CI) 95%, 6.4-10.8; vs. 12.3 months; CI 95%, 10.4-14,2; P = 0.03] and with increased progression rate (29% vs. 9%, P = 0.02). A specific EPHA2 inhibitor reverts in vitro and in vivo primary and acquired resistance to anti-ECFR therapy. EPHA2 levels are significantly associated with worse outcome in patients treated with FOLFIRI + cetuximab. These results highlight EPHA2 as a potential therapeutic target in metastatic colorectal cancer.

About 1-Phenylurea, If you have any questions, you can contact Martini, G; Cardone, C; Vitiello, PP; Belli, V; Napolitano, S; Troiani, T; Ciardiello, D; Della Corte, CM; Morgillo, F; Matrone, N; Sforza, V; Papaccio, G; Desiderio, V; Paul, MC; Moreno-Viedma, V; Normanno, N; Rachiglio, AM; Tirino, V; Maiello, E; Latiano, TP; Rizzi, D; Signoriello, G; Sibilia, M; Ciardiello, F; Martinelli, E or concate me.. Safety of 1-Phenylurea

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

COA of Formula: C7H8N2O. Tiwari, S; Arya, N; Mishra, SK; Suryaprakash, N in [Tiwari, Surbhi; Arya, Neeru; Suryaprakash, N.] Indian Inst Sci, NMR Res Ctr, Bangalore 560012, Karnataka, India; [Tiwari, Surbhi; Arya, Neeru; Suryaprakash, N.] Indian Inst Sci, Solid State & Struct Chem Unit, Bangalore 560012, Karnataka, India; [Mishra, Sandeep Kumar] Indian Inst Sci Educ & Res, Dept Phys, Pune 411008, Maharashtra, India; [Mishra, Sandeep Kumar] Indian Inst Sci Educ & Res, NMR Res Ctr, Pune 411008, Maharashtra, India published Competing HB acceptors: an extensive NMR investigations corroborated by single crystal XRD and DFT calculations in 2021, Cited 57. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

A series of N-benzoylanthranilamide derivatives have been synthesized with the substitution of competitive HB acceptors and investigated by NMR spectroscopy and single crystal XRD. The interesting rivalry for HB acceptance between (sic)C= and X (F or OMe) is observed in the investigated molecules which leads to an unusual increase in the electron density at the site of one of the NH protons, reflecting in the high field resonance in the H-1 NMR spectrum. The NMR experimental findings and single crystal XRD are further reinforced by the DFT studies.

COA of Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Tiwari, S; Arya, N; Mishra, SK; Suryaprakash, N or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Modular click chemistry libraries for functional screens using a diazotizing reagent WOS:000488832500035 published article about DIAZO TRANSFER; IMIDAZOLE-1-SULFONYL AZIDE; DIAZOTRANSFER; CYCLOADDITION; ALKYNES; AMINES; SUFEX; SAFE in [Meng, Genyi; Guo, Taijie; Ma, Tiancheng; Zhang, Jiong; Shen, Yucheng; Sharpless, Karl Barry; Dong, Jiajia] Univ Chinese Acad Sci, Ctr Excellence Mol Synth, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem,Chinese Acad Sci, Shanghai, Peoples R China in 2019, Cited 33. Product Details of 88-68-6. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Click chemistry is a concept in which modular synthesis is used to rapidly find new molecules with desirable properties(1). Copper(I)-catalysed azide-alkyne cycloaddition (CuAAC) triazole annulation and sulfur(VI) fluoride exchange (SuFEx) catalysis are widely regarded as click reactions(2-4), providing rapid access to their products in yields approaching 100% while being largely orthogonal to other reactions. However, in the case of CuAAC reactions, the availability of azide reagents is limited owing to their potential toxicity and the risk of explosion involved in their preparation. Here we report another reaction to add to the click reaction family: the formation of azides from primary amines, one of the most abundant functional groups(5). The reaction uses just one equivalent of a simple diazotizing species, fluorosulfuryl azide(6-11) (FSO2N3), and enables the preparation of over 1,200 azides on 96-well plates in a safe and practical manner. This reliable transformation is a powerful tool for the CuAAC triazole annulation, the most widely used click reaction at present. This method greatly expands the number of accessible azides and 1,2,3-triazoles and, given the ubiquity of the CuAAC reaction, it should find application in organic synthesis, medicinal chemistry, chemical biology and materials science.

Product Details of 88-68-6. About 2-Aminobenzamide, If you have any questions, you can contact Meng, GY; Guo, TJ; Ma, TC; Zhang, J; Shen, YC; Sharpless, KB; Dong, JJ or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

In 2019.0 LUNG CANCER published article about NSCLC; CHEMOTHERAPY; DOCETAXEL; SYSTEM in [Crino, Lucio; Bronte, Giuseppe; Cravero, Paola; Delmonte, Angelo] Ist Sci Romagnolo Studio & Cura Tumori IRST IRCCS, Meldola, Italy; [Bidoli, Paolo] Osped San Gerardo, Monza, Italy; [Minenza, Elisa] AO Santa Maria, Terni, Italy; [Cortesi, Enrico] Policlin Umberto 1, Rome, Italy; [Garassino, Marina C.; Proto, Claudia] Fdn IRCCS Ist Nazl Tumori, Milan, Italy; [Cappuzzo, Federico] AUSL Romagna, Ravenna, Italy; [Grossi, Francesco] IRCCS AOU San Martino IST, Genoa, Italy; [Tonini, Giuseppe] Policlin Univ Campus Biomed, Rome, Italy; [Sarobba, Maria Giuseppina] ASL 3 S Francesco, Nuoro, Italy; [Pinotti, Graziella] Osped Circolo & Fdn Macchi, Varese, Italy; [Numico, Gianmauro] AO SS Antonio & Biagio & C Arrigo, Alessandria, Italy; [Samaritani, Riccardo] Presidio Nuovo Regina Margherita, Rome, Italy; [Ciuffreda, Libero] AOU Citta Salute & Sci Torino, Turin, Italy; [Frassoldati, Antonio] Arcispedale S Anna Ferrara, Ferrara, Italy; [Bregni, Marco] Presidio Osped Busto Arsizio, Varese, Italy; [Santo, Antonio] AO Univ Integrata Verona, Verona, Italy; [Piantedosi, Francovito; Illiano, Alfonso] AO Colli, Monaldi Cotugno CTO, Naples, Italy; [De Marinis, Filippo] European Inst Oncol, Milan, Italy; [Tamberi, Stefano] Infermi Hosp, Faenza, Italy; [Giannarelli, Diana] Regina Elena Natl Canc Inst IRCCS, Rome, Italy in 2019.0, Cited 22.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8. Recommanded Product: 64-10-8

Objectives: Brain metastases are common among patients with non-squamous non-small-cell lung cancer (NSCLC) and result in a poor prognosis. Consequently, such patients are often excluded from clinical trials. In Italy an expanded access program (EAP) was used to evaluate nivolumab efficacy and safety in this sub population outside a clinical trial. Materials and methods: In this EAP, nivolumab was available for patients with non-squamous NSCLC in progression after at least one systemic treatment for stage IIIB/IV disease. Nivolumab 3 mg/kg was administered intravenously every 2 weeks. Patients with brain metastases could be included if they were asymptomatic, neurologically stable and either off corticosteroids or on a stable or decreasing dose of <= 10 mg/day prednisone. Results: 409 out of 1588 patients included had asymptomatic or controlled brain metastases. A median of 7 doses (range 1-45) were delivered. Median follow-up was 6.1 months (range 0.1-21.9). The disease control rate was 39%: 4 patients had a complete response, 64 a partial response and 96 showed stable disease. At baseline, 118 patients were on corticosteroids and 74 were undergoing concomitant radiotherapy. The median overall survival in this subpopulation was 8.6 months (95% CI: 6.4-10.8). 337 discontinued treatment for various reasons, 23 (7%) of whom due to adverse events, in line with that observed in the overall population and in previous studies. Conclusions: Our results confirm that nivolumab is active in non-squamous NSCLC patients with brain metastases, despite their poor prognosis. Its safety profile is also concordant with results in the EAP overall population and in patients with other malignancies. About 1-Phenylurea, If you have any questions, you can contact Crino, L; Bronte, G; Bidoli, P; Cravero, P; Minenza, E; Cortesi, E; Garassino, MC; Proto, C; Cappuzzo, F; Grossi, F; Tonini, G; Sarobba, MG; Pinotti, G; Numico, G; Samaritani, R; Ciuffreda, L; Frassoldati, A; Bregni, M; Santo, A; Piantedosi, F; Illiano, A; De Marinis, F; Tamberi, S; Giannarelli, D; Delmonte, A or concate me.. Recommanded Product: 64-10-8

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Linear and cyclic oligomers in PET, glycol-modified PET and Tritan (TM) used for food contact materials WOS:000590108700001 published article about POLYETHYLENE TEREPHTHALATE PET; IDENTIFICATION; MIGRATION; POLY(ETHYLENE-TEREPHTHALATE); QUANTIFICATION; POLYMERIZATION; POLYESTERS; MONOMERS in [Brenz, Fabrian; Linke, Susanne; Simat, Thomas J.] Tech Univ Dresden, Dept Chem & Food Chem, Chair Food Sci & Food Contact Mat, Dresden, Germany in 2021, Cited 39. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Formula: C7H8N2O

Polyesters are commonly used as food contact materials. During manufacture of polyesters different low molecular mass oligomers (<1000 Da) are formed in the polymer melt. These so-called non-intentionally added substances (NIAS) are potential migrants into foods. In this work, different polyester samples made of polyethylene terephthalate (PET), glycol-modified PET (PETG) and Tritan (TM) were investigated on their qualitative and quantitative oligomer composition. The analysis of acetonitrile extracts by HPLC-DAD/ESI-MS revealed the presence of about 100 linear (different combinations of hydroxyl-, carboxyl-, methyl ester end groups) and cyclic oligomers depending on the main and co-monomers. The identified oligomers were quantified in different extracts and after reprecipitation by HPLC-DAD using bis-hydroxyethylene terephthalate (BHET) as external standard. The amount of oligomers isolated by reprecipitation ranged between 0.80 and 3.4% in the respective polyester. Cyclic oligomers generally made up 90% or more of the isolated oligomers. Compared to the exhaustive extracts the leaching of oligomers into 20% ethanol (1 h, 60 degrees C) resulted in a considerable change of the oligomer distribution with a predominant detection of linear oligomers. This suggests linear oligomers to be relevant for migration into aqueous foods despite the dominant amount of extractable cyclic oligomers in polyesters. Analysis of the extractable oligomers of a PET preform and a PETG container and their corresponding raw material pellets revealed that the injection moulding process did not significantly change the amount of cyclic oligomers but did increase the amount of low molecular mass linear oligomers about twofold. Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Brenz, F; Linke, S; Simat, TJ or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Retarding frosting of an air source heat pump by using vapor-bypassed evaporation technique WOS:000662969100008 published article about DEFROSTING PERFORMANCE; CONDITIONING SYSTEM; EXCHANGER; UNIT in [Fan, Chaochao; Xiong, Tong; Yan, Gang; Yu, Jianlin; Zhang, Hao; Chu, Wenxiao; Wang, Qiuwang] Xi An Jiao Tong Univ, Dept Refrigerat & Cryogen Engn, Sch Energy & Power Engn, Xian 710049, Peoples R China; [Zhang, Hao] Guangdong Midea Refrigerat Equipment Co Ltd, Foshan 528311, Peoples R China in 2021.0, Cited 25.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8. Recommanded Product: 64-10-8

This paper presents a comparative experimental study on the frosting characteristics of an air source heat pump system that contains two operation modes, i.e., the vapor-bypassed evaporation (VB) mode and the conventional operation (CO) mode. For VB mode, a phase separator is installed inside the evaporator re-frigerant circuit to bypass vapor refrigerant, which can increase the average evaporation temperature for retarding frosting by reducing refrigerant pressure drop and decreasing the area of refrigerant inferior heat transfer coefficient region (mist flow region). According to the experimental results, under H2 con-dition (indoor: 20/15 degrees C; outdoor: 2/1 degrees C), as the initial refrigerant mass flow rate ranges 35-45 g / s , the VB mode yields 4.30-7.06% lower frost mass, 3.9-7.3% higher average heating capacity and 6.4-10.8% higher coefficient of performance (COP) over CO mode with the frosting duration of 60 min. Moreover, under H3 condition (indoor: 20/15 degrees C; outdoor:-7/-8 degrees C), the frosting duration is set as 100 min, and the VB mode obtains 9.67% lower frost mass, 7.0% higher average heating capacity and 13.3% higher COP over CO mode. Generally, the vapor-bypassed evaporation technique has a great application potential in retarding frosting and improving performance of an air source heat pump system especially under high heating capacity or low ambient temperature conditions. (c) 2021 Elsevier Ltd and IIR. All rights reserved.

Recommanded Product: 64-10-8. About 1-Phenylurea, If you have any questions, you can contact Fan, CC; Xiong, T; Yan, G; Yu, JL; Zhang, H; Chu, WX; Wang, QW or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Name: 2-Aminobenzamide. I found the field of Chemistry very interesting. Saw the article Lewis-acid-promoted cyclization reaction: synthesis of N3-chloroethyl and N3-thiocyanatoethyl quinazolinones published in 2021, Reprint Addresses Huang, GS (corresponding author), Lanzhou Univ, Dept Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide.

A Lewis-acid-promoted cyclization reaction of benzoyl chlorides with 2-(4,5-dihydrooxazol-2-yl)anilines, which can offer a series of N3-chloroethyl quinazolinones, is disclosed. The reaction is compatible with the functional groups of the substrates; environment-friendly AlCl3 is probably the chloride source. Moreover, the addition of NH4SCN can also produce a range of N3-thiocyanatoethyl quinazolinones in moderate-to-good yields.

Name: 2-Aminobenzamide. About 2-Aminobenzamide, If you have any questions, you can contact Hu, FP; Zhang, MM; Huang, GS or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Synthesis of novel 3-(quinazol-2-yl)-quinolines via SNAr and aluminum chloride-induced (hetero) arylation reactions and biological evaluation as proteasome inhibitors WOS:000527104200011 published article about NONCOVALENT INHIBITION; INDUCED HETEROARYLATION; PRIVILEGED SCAFFOLD; 20S PROTEASOME; CANCER; QUINOLINE; IDENTIFICATION; QUINAZOLINES; ALLOSTERY; TMC-95A in [Boualia, Imen; Debache, Abdelmadjid; Boulcina, Raouf] Univ Freres Mentouri Constantine, Lab Synthese Mol Interets Biol, Constantine 25000, Algeria; [Boualia, Imen; Roisnel, Thierry; Berree, Fabienne; Vidal, Joelle; Carboni, Bertrand] Univ Rennes, ISCR, CNRS, UMR 6226, F-35000 Rennes, France; [Boulcina, Raouf] Univ Mostefa Benboulaid Batna 2, Dept Sci & Tech, Fac Technol, Batna 05000, Algeria in 2020, Cited 45. Safety of 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

A new series of 3-(quinazol-2-yl)-quinolines was synthesized by SNAr reaction from easily prepared 4-chloro-2-(2-chloroquinolin-3-yl)quinazolines and a range of phenols and thiophenol as nucleophiles. The AlCl3-mediated CC bond formation was also successfully exploited to introduce aryl and hereroaryl substituents on one or both heterocyclic units. These procedures afford efficient syntheses of polysubstituted 3-(quinazol-2-yl)-quinolines in few steps and high yields. Some of these polysubstituted 3-(quinazol-2-yl)-quinolines inhibit the human 20S proteasome. (C) 2020 Elsevier Ltd. All rights reserved.

About 2-Aminobenzamide, If you have any questions, you can contact Boualia, I; Debache, A; Boulcina, R; Roisnel, T; Berree, F; Vidal, J; Carboni, B or concate me.. Safety of 2-Aminobenzamide

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Authors Martini, G; Cardone, C; Vitiello, PP; Belli, V; Napolitano, S; Troiani, T; Ciardiello, D; Della Corte, CM; Morgillo, F; Matrone, N; Sforza, V; Papaccio, G; Desiderio, V; Paul, MC; Moreno-Viedma, V; Normanno, N; Rachiglio, AM; Tirino, V; Maiello, E; Latiano, TP; Rizzi, D; Signoriello, G; Sibilia, M; Ciardiello, F; Martinelli, E in AMER ASSOC CANCER RESEARCH published article about ACQUIRED-RESISTANCE; CAPRI-GOIM; PLUS CETUXIMAB; INHIBITOR; MUTATIONS in [Martini, Giulia; Cardone, Claudia; Vitiello, Pietro Paolo; Belli, Valentina; Napolitano, Stefania; Troiani, Teresa; Ciardiello, Davide; Della Corte, Carminia Maria; Morgillo, Floriana; Matrone, Nunzia; Ciardiello, Fortunato; Martinelli, Erika] Univ Campania L Vanvitelli, Med Oncol, Dept Precis Med, Via Pansini 5, I-80131 Naples, Italy; [Sforza, Vincenzo] Fdn Pascale, IRCCS, Ist Nazl Tumori, Dept Clin Expt Thorac Oncol, Naples, Italy; [Papaccio, Gianpaolo; Desiderio, Vincenzo; Tirino, Virginia] Univ Campania Luigi Vanvitelli Napoli, Dept Expt Med, Naples, Italy; [Paul, Mariel C.; Moreno-Viedma, Veronica; Sibilia, Maria] Med Univ Vienna, Comprehens Canc Ctr, Dept Med 1, Inst Canc Res, Borschkegasse 8a, Vienna, Austria; [Normanno, Nicola; Rachiglio, Anna Maria] Fdn Pascale, IRCCS, Ist Nazl Tumori, Cell Biol & Biotherapy Unit, Naples, Italy; [Maiello, Evaristo; Latiano, Tiziana Pia; Rizzi, Daniele] Hosp Casa Sollievo Della Sofferenza San Giovanni, Med Oncol, San Giovanni Rotondo, Italy; [Signoriello, Giuseppe] Univ Campania L Vanvitelli, Biostat, Dipartimento Salute Mentale & Fis & Med Prevent, Naples, Italy in 2019.0, Cited 24.0. Application In Synthesis of 1-Phenylurea. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8

The EPHA2 tyrosine kinase receptor is implicated in tumor progression and targeted therapies resistance. We evaluated EPHA2 as a potential resistance marker to the antiepidermal growth factor receptor (EGFR) monoclonal antibody cetuximab in colorectal cancer. We studied activation of EPHA2 in a panel of human colorectal cancer cell lines sensitive or resistant to anti-EGFR drugs. The in vitro and in vivo effects of ALW-II-41-27 (an EPHA2 inhibitor) and/or cetuximab treatment were tested. Fonnalin-fixed paraffin-embedded tumor specimens from 82 RAS wild-type (WV) metastatic colorectal cancer patients treated with FOLFIRI + cetuximab as first-line therapy in the CAPRI-COIM trial were assessed for EPHA2 expression by immunohistochemistry and correlated with treatment efficacy. EPHA2 was differentially activated in colorectal cancer cell lines. Combined treatment with ALW-II-41-27 plus cetuximab reverted primary and acquired resistance to cetuximab, causing cell growth inhibition, inducing apoptosis and cell-cycle G1-G2 arrest. In tumor xenograft models, upon progression to cetuximab, ALW-II-41-27 addition significantly inhibited tumor growth. EPHA2 protein expression was detected in 55 of 82 tumor samples, frequently expressed in less-differentiated and left-sided tumors. High levels of EPHA2 significantly correlated with worse progression-free survival [8.6 months; confidence interval (CI) 95%, 6.4-10.8; vs. 12.3 months; CI 95%, 10.4-14,2; P = 0.03] and with increased progression rate (29% vs. 9%, P = 0.02). A specific EPHA2 inhibitor reverts in vitro and in vivo primary and acquired resistance to anti-ECFR therapy. EPHA2 levels are significantly associated with worse outcome in patients treated with FOLFIRI + cetuximab. These results highlight EPHA2 as a potential therapeutic target in metastatic colorectal cancer.

About 1-Phenylurea, If you have any questions, you can contact Martini, G; Cardone, C; Vitiello, PP; Belli, V; Napolitano, S; Troiani, T; Ciardiello, D; Della Corte, CM; Morgillo, F; Matrone, N; Sforza, V; Papaccio, G; Desiderio, V; Paul, MC; Moreno-Viedma, V; Normanno, N; Rachiglio, AM; Tirino, V; Maiello, E; Latiano, TP; Rizzi, D; Signoriello, G; Sibilia, M; Ciardiello, F; Martinelli, E or concate me.. Application In Synthesis of 1-Phenylurea

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem