EZM 2302 - 10mM in DMSO , CAS No.1628830-21-6

CAS: 1628830-21-6 Cat. No.: E655335 Formule: C₂₉H₃₇ClN₆O₅ Poids moléculaire: 585.09

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Vue d’ensemble

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

In Vitro

EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC 50 =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 IC 50 values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC 50 values of less than 100 nM in 9 of 15 cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

IC50& Target:IC50: 6 nM (CARM1)

Specifications

Spécifications et pureté

10mM in DMSO

Mécanismes biochimiques et physiologiques

EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 ( CARM1 ) with an IC 50 of 6u2009nM.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Noms et identifiants

• Isomères SMILES: CC1=C(N=C(N=C1N2CC3(C2)CCN(CC3)C(=O)OC)C4=C(C=CC(=C4)OC[C@@H](CNC)O)Cl)C5=C(ON=C5C)C
• Poids moléculaire: 585.09