GSK3359088 manufacturers
- EZM 2302
-
- $2.00
-
2026-08-25
- CAS:1628830-21-6
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100kg
- EZM 2302
-
- $68.00
-
2026-07-14
- CAS:1628830-21-6
- Purity: 97.47%
- Supply Ability: 10g
|
| | GSK3359088 Basic information |
| Product Name: | GSK3359088 | | Synonyms: | GSK3359088;EZM2302 (GSK3359088);EZM2302;EZM-2302;EZM 2302;CS-2741;2,7-Diazaspiro[3.5]nonane-7-carboxylic acid, 2-[2-[2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl]-6-(3,5-dimethyl-4-isoxazolyl)-5-methyl-4-pyrimidinyl]-, methyl ester;Methyl 2-(2-(2-chloro-5-((R)-2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate;Methyl 2-[2-[2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl]-6-(3,5-dimethyl-4-isoxazolyl)-5-methyl-4-pyrimidinyl]-2,7-diazaspiro[3.5]nonane-7-carboxylate;inhibit,Inhibitor,EZM2302,Histone Methyltransferase,EZM 2302,EZM-2302 | | CAS: | 1628830-21-6 | | MF: | C29H37ClN6O5 | | MW: | 585.09 | | EINECS: | | | Product Categories: | | | Mol File: | 1628830-21-6.mol |  |
| | GSK3359088 Chemical Properties |
| Boiling point | 705.8±60.0 °C(Predicted) | | density | 1.36±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:91.0(Max Conc. mg/mL);155.53(Max Conc. mM)
DMSO:91.0(Max Conc. mg/mL);155.53(Max Conc. mM) | | form | A solid | | pka | 13.79±0.20(Predicted) | | color | White to off-white | | InChIKey | OWCOTUVKROVONT-HXUWFJFHSA-N | | SMILES | C1C2(CCN(C(OC)=O)CC2)CN1C1C(C)=C(C2=C(C)ON=C2C)N=C(C2=CC(OC[C@H](O)CNC)=CC=C2Cl)N=1 |
| | GSK3359088 Usage And Synthesis |
| Uses | EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression[1]. | | in vivo | EZM 2302 (37.5, 75, 150, 300 mg/kg; p.o.; twice daily for 21 days) shows anti-tumor activity in mouse[1].
Pharmacokinetic Parameters of EZM 2302 in CD-1 mouse and Sprague-Dawley rat[1].
| Parameters | IV(CD-1 mouse) | PO(CD-1 mouse) | IV (Sprague-Dawley rat) | PO (Sprague-Dawley rat) | | Dose (mg/kg) | 2 | 10 | 2 | 10 | | Blood:plasma ratio | 1.2 | 1.2 | 2.6 | ND | | Cmax(ng/mL) | | 177 | | 113±22.4 | | Tmax(h) | | 2.00 | | 2.00 | | AUC0-last(ng.h/mL) | 767 | 568 | 352±30.6 | 453±89.3 | | AUC0-inf(ng.h/mL) | 772 | 577 | 372±43.3 | 487±102 | | t1/2(h) | 4.22 | 4.55 | 6.21±1.65 | 6.64±1.41 | | Vss(L/kg) | 6.53 | | 35.6±1.30 | | | CL (mL/min/kg) | 43.2 | | 90.5±10.5 | | | Fa*Fg (%) | | ND | | 80.7 | | F (%) | | 15.0 | | 26.2±5.45 |
CD-1 mouse and Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po [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. DOI:10.1038/s41598-017-18446-z |
| | GSK3359088 Preparation Products And Raw materials |
|