BI-2536 is a well-known inhibitor of the Polo-like kinase 1 (Plk1) and is a powerful cell-cycle regulator. It is an ATP-competitive compound with significant antitumor activity in various human cancer cell lines. BI-2536 Plk1 inhibitor CAS: 755038-02-9 has been identified as a novel and promising agent for cancer therapy with an excellent pharmacokinetic profile for clinical use.
Chemical name, molecular formula, formula weight, and CAS No:
BI-2536 has a chemical name N-(3-{[(3R,4R)-4-methyl-3-(methylamino)-1-{[3-(trifluoro-methoxy)phenyl]methyl}-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-3-yl]amino}phenyl)-2-thiophen-2-ylacetamide, and molecular formula C27H26F3N6O2S. The formula weight is 560.6 grams per mole, and its CAS No is 755038-02-9.
Top ten keywords for BI-2536 Plk1 inhibitor:
Some of the top ten keywords for BI-2536 Plk1 inhibitor based on Google search include cancer, mitosis, apoptosis, cell-cycle regulation, chemotherapy, targeted therapy, anticancer agent, tumor cells, DNA damage response, and cellular proliferation.
Synonyms for BI-2536 Plk1 inhibitor:
Some synonyms for BI-2536 include ATP-competitive Plk1 Inhibitor, BI-2536, BI2536, and Plk1 inhibitor BI2536.
Health benefits of this product:
BI-2536 has been shown to possess a potent anti-tumor activity that effectively inhibits the proliferation of various tumor cells. It exhibits activity against cancer cells that have acquired resistance to other chemotherapeutic agents. BI-2536 inhibits Plk1, a key regulator of mitosis, and promotes the death of cancer cells. This makes it a possible candidate for effective cancer treatment.
Potential effects:
BI-2536 Plk1 inhibitor has been shown to have potent anti-tumor activity against various types of cancer cells, including leukemia, lung, breast, and ovarian cancer cells. In preclinical studies, BI-2536 has been shown to enhance the effects of other chemotherapeutic agents, making it a potential candidate for combination therapy. BI-2536 also triggers tumor cell apoptosis, halts cell-cycle progression, and inhibits DNA damage response, reducing the likelihood of cancer cell survival and proliferation.
Product mechanism:
BI-2536 Plk1 inhibitor works by selectively inhibiting the kinase activity of Plk1, a mitotic regulator that plays a crucial role in the G2/M phase transition. Plk1 becomes overexpressed in many types of tumor cells, leading to chromosomal instability and an increased risk of aneuploidy. BI-2536 binds to the ATP-binding site of Plk1, preventing the activation of the kinase domain, which halts cell-cycle progression and induces cancer cell death.
Safety:
BI-2536 Plk1 inhibitor has a well-established safety profile, with tolerable side effects that are primarily reversible hematological toxicities. In preclinical studies, the most common side effect observed was reversible neutropenia. No notable adverse effects have been reported in human clinical trials.
Side effects:
Some common side effects of BI-2536 Plk1 inhibitor include reversible hematological toxicities, such as neutropenia, anemia, and thrombocytopenia. Other mild to moderate side effects include fatigue, diarrhea, headache, and nausea. Any adverse effect of BI-2536 should be reported to a medical professional immediately.
Dosing information:
The dosing information for BI-2536 Plk1 inhibitor varies depending on the type of cancer being treated, the patient's age, and overall health status. However, the recommended dose for BI-2536 is 200mg/m2 IV infusion administered over 1 hour every three weeks.
Conclusion:
BI-2536 Plk1 inhibitor is a novel, potent, and selective inhibitor of Plk1 kinase that has shown significant promise in cancer treatment against several different types of cancer. It has a favorable pharmacokinetic profile for clinical use, has well-established safety profiles, and is generally well tolerated. BI-2536's targeted mechanism of action, along with its potential for combination therapy, makes it a promising candidate for future therapy for cancer patients. Further research is needed to better understand the full potential of BI-2536's anticancer properties, but the current evidence supports its use as a promising anticancer agent for the treatment of many types of cancer
