Product Details
| Product Name: EZM 2302 | CAS No.: 1628830-21-6 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: 100kg | Release date: 2026/07/02 |
| Lead time: in stock | Packaging: bag/bottle/drum//IBC, as request |
| Packaging: By sea, by air, by express | Origin: Manufacturer |
| Name: Tina |
PRODUCT INFORMATION
| Name | GSK3359088 |
|---|---|
| Synonym | More Synonyms |
| Description | EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6?nM. |
|---|---|
| Related Catalog | Signaling Pathways >> Others >> Others Research Areas >> Cancer |
| Target | IC50: 6?nM (CARM1)[1] |
| In Vitro | EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC50=6?nM) with broad selectivity against other histone methyltransferases. Treatment of MM cell lines with EZM 2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC50 values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC50 values of less than 100?nM in 9 of 15 cell lines[1]. |
| In Vivo | EZM 2302 is stable in human hepatocytes (CL<3?mL/min/kg), and moderately binds to human, mouse and rat plasma proteins with a mean fraction unbound of 0.66, 0.46 and 0.74, respectively. In mouse and rat, the plasma clearance (CL) is 43 and 91?mL/min/kg, respectively. EZM 2302 shows dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM 2302 dose groups measured on day 21 show significant decreases in tumor growth compared to vehicle[1]. |
| Cell Assay | Cultured cells in linear/log phase growth are split to a seeding density of 2e5 cells/mL in 2–20mLs of media, depending on the yield required at the end of the growth period. EZM 2302 is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96?hours. At the conclusion of each treatment period, cells are harvested by centrifugation (5?minutes, 1200?rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing[1]. |
| Animal Admin | Rats[1] Male Sprague-Dawley rats (n=3) are treated with a single dose of EZM2302 at 2?mg/kg by intravenous (i.v.) injection and 10?mg/kg by oral gavage administration (p.o.; mouse only), formulated in 5% dextrose in water, pH 3.5. An additional group of rats, cannulated in both the jugular and portal veins are dosed by oral gavage (10?mg/kg, in 0.5% methylcellulose in water). Approximately 110?μL of blood is taken from the animals by retro-orbital bleeding (mouse), tail vein (rat i.v.) or both jugular and portal vein sampling (rat p.o.) at pre-specified time intervals. The 2?h samples are split for parallel determination of blood and plasma concentration[1]. Mice[1] RPMI-8226 cells are inoculated at 5×106 cells/mouse and treatment began when the mean tumor sizes reach 120?mm3 (28 days post-inoculation). CB-17 SCID Mice are assigned into groups using a randomized block design. EZM2302 or vehicle (0.5% methylcellulose in water) is administered orally BID at a dose volume of 37.5, 75, 150, or 300?mg/kg for 21 days. Body weights are measured twice a week for the duration of the study. Tumor size is measured twice weekly in two dimensions using a caliper, and the volume is expressed in cubic millimeters. Animals are euthanized 3?hours post-final dose, with blood and tissues collected for analysis[1]. |
| References | [1]. Drew AE, et al. Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma. Sci Rep. 2017 Dec 21;7(1):17993. |
| Molecular Formula | C29H37ClN6O5 |
|---|---|
| Molecular Weight | 585.09 |
| Storage condition | 2-8℃ |
| GSK 3359088 |
| EZM 2302 |
Company Profile
Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions.
Our Company
Our Advantage
Rich experience
Our products have been exported to many countries, including Germany, Spain, the United Kingdom, the United States, Australia, the Middle East, Asia, and more. We have received highly positive feedback from our clients and have established long-term friendly cooperative relationships with them.
Excellent quality, purity, and competitive price
Excellent quality is one of the cornerstones of our success. We welcome ordering samples for quality testing.
Safe and fast delivery
We will arrange shipment of spot products as soon as we receive payment.
Customized products are determined based on the synthesis time of different products.
Excellent pre-sales and after-sales service
Pre sales:
We are committed to providing the most favorable quotes and detailed information about our products and company.
after-sale service:
We assist buyers in customs clearance by providing necessary documents and information.
If there is any dispute over product quality, we are committed to providing the best solution.
? Packaging:
1kg/bag, 25kg/drum, 50kg/drum, 180kg/drum, 200kg/drum, 1T/bag/drum, standard export packaging or packaging required by customers
? Shipping
? Delivery:
Within 7 days after receiving your payment
Contact information
For more details, pls contact us freely.
Contact name: Tina
Email address: Tina@fdachem.com
Mob: 86 13213167925
WhatsApp/Skype/Wechat/LINE: 86 15225627621
China