TG101209 (TG-101209) (CAS: 936091-14-4) is a small-molecule inhibitor of Janus kinase 2 (JAK2), developed by TargeGen for the treatment of various cancers, such as myeloproliferative neoplasms and solid tumors. JAK2 plays a critical role in cell signaling and proliferation.
Chemical name: N-(cyanomethyl)-4-(2-((4-morpholin-4-ylphenyl)amino)pyrimidin-4-ylamino)benzamide
Molecular formula: C24H25N7O2
Formula weight: 427.51 g/mol
CAS No: 936091-14-4
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Health benefits of this product: TG101209 has shown potential in preclinical and clinical studies for the treatment of various cancers, particularly myeloproliferative neoplasms and solid tumors. It works by inhibiting the activity of JAK2, which is involved in cell signaling and proliferation. By blocking these receptors, TG101209 can potentially induce apoptosis and inhibit tumor growth.
Potential effects: TG101209 has demonstrated efficacy in reducing tumor growth and inducing remission in myeloproliferative neoplasms and solid tumors in preclinical and clinical studies. It has also shown potential in combination with other anti-cancer agents, such as chemotherapy and radiation therapy. However, more research is needed to determine its full potential and efficacy in different types of cancers.
Product mechanism: TG101209 inhibits the activity of Janus kinase 2 (JAK2), which is involved in cell signaling and proliferation. JAK2 is a key mediator of cytokine signaling, including those that promote cell growth and survival. Mutations or overexpression of JAK2 are associated with various cancers, particularly myeloproliferative neoplasms and solid tumors. As a small-molecule inhibitor, TG101209 binds to the ATP-binding site of JAK2, preventing its activation and downstream signaling pathways that promote cancer cell growth and survival. By inhibiting these receptors, TG101209 can induce apoptosis and inhibit tumor growth.
Safety: TG101209 has been evaluated in several preclinical and clinical studies involving hundreds of patients with different types of cancers. Overall, it has been well-tolerated, with manageable side effects. The most common adverse events reported were fatigue, headache, and diarrhea. More severe side effects, such as thrombocytopenia and anemia, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of TG101209 include fatigue, headache, and diarrhea. These symptoms are usually mild or moderate and can be managed with supportive care or dose modifications. Less common but more severe side effects may include thrombocytopenia and anemia, which may require prompt medical intervention. Patients should be monitored closely for these adverse events and receive appropriate medical intervention if necessary.
Dosing information: The recommended dose of TG101209 varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 320 to 680 mg have been evaluated, either as a single agent or in combination with other drugs. Treatment duration also varies and can range from a few weeks to several months, depending on the response and tolerability. Patients should follow their doctor's instructions regarding dosing, administration, and monitoring.
Conclusion: TG101209 (TG-101209) (CAS: 936091-14-4) is a promising small-molecule inhibitor of Janus kinase 2 (JAK2) that has shown potential in preclinical and clinical studies for the treatment of various cancers, particularly myeloproliferative neoplasms and solid tumors. Its mechanism of action involves blocking key receptors involved in cell signaling and proliferation, leading to apoptosis and reduced tumor growth. Although it has been generally well-tolerated, it may cause some side effects that should be monitored closely. Further research is needed to determine its full potential and efficacy in different types of cancers.
