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CO-1686 hydrobromide is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M (IC50=21 nM).IC50 value: 21.5±1.7 nM (EGFRL858R/T790M), 303.3 ± 26.7 nM (EGFRWT)in vitro: CO-1686 is a potent inhibitor of EGFR L858R/T790M kinase (kinact/Ki = (2.41 ± 0.30) x 105 M-1s-1) and is approximately 22-fold selective over WT EGFR (kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1). CO-1686 potently inhibited proliferation in the mutant-EGFR NSCLC cellswith GI50 values ranging from 7 - 32 nM. In comparison, the GI50 value for A431 cells, an epidermoid cell line that is driven by amplified WT EGFR(19), was 547 nM. Two cell lines expressing WT EGFR in the presence of an N- or KRAS mutation (NCI-H1299 and NCI-H358,respectively) were inhibited by CO-1686 at a concentration of 4275 and 1806 nM, respectively.in vivo: CO-1686 displays high oral bioavailability (65%) and a relatively long half-life of 2.6 hours when dosed at 20 mg/kg. Tumor-bearing mice were dosed orally once daily with CO-1686 as single agent and its effect on tumor growth was determined in several EGFR dependent xenograft models. Continuous oral dosing of CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models examined. At 100 mg/kg/day CO-1686 causs tumor regressions in two Erlotinib-resistant models expressing the L858R/T790M EGFR mutation, the NCI-H1975 cell line xenograft and the patient-derived lung tumor xenograft (PDX) LUM1868, while Erlotinib had no inhibitory effect on tumor growth.
Quiflapon sodium is a synthetic compound that belongs to the class of selective 5-lipoxygenase inhibitors. It is a potent anti-inflammatory agent that has been extensively studied for its potential therapeutic applications in various diseases.
Favipiravir is an antiviral drug that has gained attention due to its potential use in the treatment of viral infections, including influenza and COVID-19. It was first developed in Japan in 2014 and has since been approved for use in several countries. This paper will provide an overview of Favipiravir, including its method of synthesis or extraction, chemical structure and biological activity, biological effects, applications, and future perspectives and challenges.
Naloxone is a medication used to reverse the effects of opioid overdose. It is an opioid antagonist that works by binding to the same receptors in the brain that opioids bind to, thereby reversing the effects of the opioids. Naloxone has been used for decades in emergency medicine and is now being used more widely in the community to prevent opioid overdose deaths. This paper will provide an overview of the synthesis and extraction methods of naloxone, its chemical structure and biological activity, its biological effects, applications in medical, environmental, and industrial research, and future perspectives and challenges.
Leucovorin, also known as folinic acid, is a synthetic form of folate, a B-vitamin essential for DNA synthesis and cell division. It is commonly used in combination with chemotherapy drugs to enhance their efficacy and reduce their toxicity. Leucovorin is also used in the treatment of certain types of anemia and in the prevention of birth defects.
Asparagusic acid is a sulfur-containing compound found in asparagus, which is responsible for the unique odor and taste of the vegetable. It has gained significant attention in recent years due to its potential therapeutic and environmental applications. This paper aims to provide a comprehensive review of asparagusic acid, including its method of synthesis or extraction, chemical structure and biological activity, biological effects, applications, and future perspectives and challenges.
4,4'-Diacetamidodiphenylmethane, also known as DADPM, is a chemical compound that belongs to the class of diarylmethanes. It is a white crystalline solid that is soluble in organic solvents such as ethanol and acetone. DADPM has been studied for its potential biological and industrial applications due to its unique chemical structure.
Methotrexate is a widely used drug in the treatment of various diseases, including cancer, autoimmune disorders, and ectopic pregnancy. It is a folate antagonist that inhibits the synthesis of DNA, RNA, and proteins, leading to the death of rapidly dividing cells. Methotrexate has been in use for over 60 years and has proven to be effective in treating a range of diseases. This paper will discuss the method of synthesis or extraction, chemical structure and biological activity, biological effects, applications, future perspectives, and challenges of methotrexate.