5-iodo-1H-pyrazolo[3,4-b]pyridin-3-amine cas 1392152-87-2 support customized synthesis

Its generic name is Tazemetostat, and its trade name is Tazverik.
Below, we will provide a detailed introduction to this compound:
1. Basic Information
· CAS Number: 1392152-87-2
· Chemical Name: N-[(4,6-diamino-2,5-dihydro-1,3,5-triazine-2-yl)methyl]-4-fluorobenzoamide
· Generic Name: Tazemetostat (Tazestat)
· Trade Name: Tazverik
· Molecular Formula: C₃₄H₄₄N₄O₄
· Molecular Weight: 572.74 g/mol
· Development Code: EPZ-6438
2. Pharmacological Effects and Targets
Tazemetostat is a novel, highly selective, orally bioavailable inhibitor of the histone methyltransferase EZH2.
· The function of EZH2: EZH2 is an enzyme whose main function is to add methyl groups (H3K27me3) to the lysine at position 27 of histone H3. This epigenetic mark is usually associated with the "off" signal for gene transcription, meaning it inhibits the expression of certain genes.
· Abnormalities in cancer: In many cancers (such as follicular lymphoma, epithelioid sarcoma, etc.), the function of EZH2 becomes abnormally active or undergoes mutations. This leads to its excessive inhibition of some tumor suppressor genes that should be normally expressed, allowing cancer cells to proliferate and survive uncontrollably.
· Mechanism of Tazemetostat: Tazemetostat inhibits the activity of EZH2, reducing the level of H3K27me3, thereby relieving the inhibition on tumor suppressor genes and reactivating their expression. Eventually, it induces cancer cell differentiation, apoptosis (programmed death), and inhibits their growth.
3. Indications (Approval Status)
Tazemetostat has been approved by the US Food and Drug Administration (FDA) for the treatment of the following diseases:
1. Epithelioid sarcoma:
· Applicable for adult and pediatric patients (aged 16 and above) with metastatic or locally advanced epithelioid sarcoma who are not suitable for complete resection.
2. Follicular lymphoma:
· Applicable for adult patients with relapsed or refractory follicular lymphoma, whose tumors are confirmed as EZH2 mutation positive by FDA-approved testing methods.
· Also applicable for adult patients with relapsed or refractory follicular lymphoma who do not have satisfactory alternative treatment options.
4. Research and Development and Business Background
· Research and Development Company: It was developed by Epizyme Company (which has since been acquired by Imprevance).
· Importance: It is the world's first EZH2 inhibitor to be approved for market by the FDA, representing an important milestone in the field of epigenetic therapy for cancer treatment.
5. Key Features
· Targeted therapy: Targeted at specific epigenetic targets, it falls within the scope of precision medicine.
· Oral administration: Convenient for patients to use, improving their quality of life.
· New mechanism of action: Provides new treatment options for patients who are unresponsive to traditional chemotherapy.
Summary

CAS 1392152-87-2 (Tazemetostat) is a landmark targeted anti-cancer drug. It reverses the oncogenic epigenetic alterations by inhibiting EZH2, providing an effective approach for the treatment of certain types of epithelial sarcomas and follicular lymphomas. Its success not only brings hope to patients but also significantly promotes the development of epigenetic drug research.