EZM 2302是共激活因子相关的精氨酸甲基转移酶1 (CARM1) 制剂， IC₅₀值为6 nM。

EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC 50 of 6?nM.

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IC50: 6?nM (CARM1)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (170.91 mM; Need ultrasonic)配制储备液