EPZ-6438
Appearance: White or off-white crystalline powder
Standard: in-house
Application: Lab research
Supply Ability: 1000g per month
Purity: ≥98%
Payment: T/T, LC or DA
Delivery Time: Ready Stock in Local Warehouse, 1-3 days
Origin: China
Shipping: DHL, FedEx, TNT, EMS, By Sea, By Air
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Product Introduction
We supply Tazemetostat (EPZ-6438)
We're pleased to offer EPZ-6438 for your exploration needs. Tazemetostat API also know as EPZ-6438. it is a potent and picky asset of EZH2, a histone methyltransferase constantly overexpressed in numerous cancers. It has demonstrated significant antitumor exertion in preclinical models and is presently being estimated in clinical trials for colorful types of cancer. it is of high chastity and quality, and is available in colorful amounts to meet your exploration needs. communicate us moment to learn further about it and how it can advance your exploration in cancer biology and remedy.
What's EPZ-6438?
Tazemetostat( EPZ-6438) is a new remedial agent developed by Epizyme that targets the EZH2 histone methyltransferase enzyme. EZH2 plays a significant part in the development of several types of cancer, making it an seductive target for remedial intervention. it is specifically designed to inhibit EZH2, thereby precluding the propagation of cancer cells and promoting apoptosis.
it is being studied for the treatment of multiple types of cancer, includingnon-Hodgkin carcinoma, solid excrescences, and other blood cancers. In clinical trials, it has demonstrated strong exertion in cases with a variety of solid excrescences and hematologic malice.
Unlike traditional chemotherapy, which isnon-specific and can beget damage to healthy apkins, it is designed to specifically target cancer cells. The targeted nature of Tazemetostat makes it a promising treatment option for cases who may not have responded to other curatives or may be suffering from regressed or refractory complaint.
it has also shown promising results in combination with other cancer treatments, similar as PD- 1 impediments, which may increase its efficacity in specific patient populations. it is administered orally, which is a accessible and cost-effective administration system.
In summary, it is a new remedial agent developed to specifically target EZH2-positive cancers. It has demonstrated emotional clinical exertion and is a promising treatment option for cases with multiple types of cancer. it is poised to come an important addition to the magazine of cancer treatments, furnishing new stopgap for cases and their families.
Basic Information
Product Name: Tazemetostat (EPZ-6438)
CAS: 1403254-99-8
MF:C34H44N4O4
MW:572.74
MDL No.:MFCD24849415
Structural formula:
Origin: China
Application: Lab research
Delivery Time: in stock
Technical Specification
ITEMS |
STANDARDS |
RESULTS |
Appearance |
White or off-white crystalline powder |
Off-white crystalline powder |
Identification |
By IR |
Complies |
RT under chirality should complies |
Complies |
|
Chloride: it gives a reaction of chloride |
Complies |
|
Water |
3.0%~4.5% |
3.4% |
Melting Point |
198.0~202.0ºC |
199.8~200.5ºC |
Residue on Ignition |
≤0.2% |
0.08% |
Heavy Metals |
≤10ppm |
Complies |
Related Substances |
Individual Impurities:≤0.5% |
0.15% |
Total Impurities:≤1.0% |
0.22% |
|
Assay (on dry basis) |
98.0%~102.0% |
101.2% |
Conclusion:It complies to prescribed enterprise standard. |
Package 1g, 5g, 10g or according to your demands
Storage conditions: Preserve in tightly closed container -20°C
Shelf Life 24 months
Biological activity
EPZ-6438 is a small patch asset that targets the histone methyltransferase enzyme EZH2. EZH2 is a critical element of the Polycomb cathartic complex 2( PRC2), which is responsible for the regulation of chromatin structure and gene expression. Overexpression of EZH2 has been observed in several cancer types, and has been associated with poor case prognostic. thus, targeting EZH2 with it has the implicit to inhibit cancer cell growth and proliferation.
it has been shown to have potent inhibitory goods on EZH2 in preclinical studies. In vitro and in vivo trials have demonstrated that it can reduce EZH2- intermediatedtri-methylation of histone H3 lysine 27( H3K27), leading to a drop in the cathartic chromatin structure and an increase in gene expression. This effect is observed in cells with wild- type EZH2 as well as EZH2 mutations that are generally set up in certain cancer types.
Several clinical trials have been conducted to estimate the safety and its efficacity in cases with advanced solid excrescences, hematologic malice, and certain inheritable diseases that involve abnormalities in EZH2. The results of these studies have shown promising response rates and manageable safety biographies, indicating a favorable remedial indicator for it.
Overall, it is a largely specific asset of EZH2 that has demonstrated potent inhibitory goods on EZH2- intermediated histone methylation and gene expression. Clinical studies have shown pledge in the treatment of a variety of cancer types and inheritable diseases, making it a promising remedial agent for unborn clinical development.
Application
Tazemetostat API is a small patch asset of EZH2, a histone methyltransferase enzyme that's overexpressed in colorful cancers. By inhibiting EZH2, it blocks the methylation of histone H3 lysine 27, leading to a drop in gene recap and eventually halting cancer cell growth.
it has demonstrated promising results in preclinical and clinical studies for the treatment of colorful cancer types, including verbose large B- cell carcinoma, follicular carcinoma, mesothelioma, and synovial sarcoma. In a Phase II clinical trial, it showed an overall response rate of 71 in cases with EZH2- shifted follicular carcinoma.
it is generally well- permitted, with the most common side goods being fatigue, nausea, and dropped appetite. It's administered orally, making it accessible for cases to take at home.
Overall, it represents a promising new option in the treatment of colorful cancers, particularly those driven by EZH2 mutations. Ongoing exploration and clinical trials continue to explore the full eventuality of this innovative medicine.
In vitro research
it attention dependently reduces overall H3K27Me3 situations in wild- type or SMARCB1 mutant cells and induces strong anti proliferative goods in MRT cell lines with SMARCB1 removed, with an IC50 range of 32nM to 1000nM. it induces gene expression and cell cycle inhibition in neuronal isolation, while also inhibiting Hedgehog pathway genes, MYC, and EZH2. In several EZH2 mutant carcinoma cells, its anti proliferative effect is enhanced by prednisone or dexamethasone.
In vivo research
Subcutaneous injection of G401 xenograft into SCID mice redounded in EPZ-6438 causing excrescence counterpoise and significant excrescence growth detention during administration, with minimum impact on body weight.
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