GSK3359088
- Product Name
- GSK3359088
- CAS No.
- 1628830-21-6
- Chemical Name
- GSK3359088
- Synonyms
- CS-2741;EZM2302;GSK3359088;EZM2302 (GSK3359088);EZM 2302, 10 mM in DMSO;EZM2302;EZM-2302;EZM 2302;inhibit,Inhibitor,EZM2302,Histone Methyltransferase,EZM 2302,EZM-2302;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;methyl 2-(2-{2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl}-6-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate
- CBNumber
- CB93364258
- Molecular Formula
- C29H37ClN6O5
- Formula Weight
- 585.09
- MOL File
- 1628830-21-6.mol
GSK3359088 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 29954
- Product name
- EZM2302
- Packaging
- 1mg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 29954
- Product name
- EZM2302
- Packaging
- 10mg
- Price
- $601
- Updated
- 2024/03/01
- Product number
- 29954
- Product name
- EZM2302
- Packaging
- 5mg
- Price
- $319
- Updated
- 2024/03/01
- Product number
- 3748EB
- Product name
- Methyl2-[2-[2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methylpyrimidin-4-yl]-2,7-diazaspiro[3.5]nonane-7-carboxylate
- Packaging
- 5mg
- Price
- $452
- Updated
- 2021/12/16
- Product number
- CS-0034242
- Product name
- EZM2302
- Purity
- 99.49%
- Packaging
- 5mg
- Price
- $200
- Updated
- 2021/12/16
GSK3359088 Chemical Properties,Usage,Production
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 |
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
Raw materials
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View Lastest Price from GSK3359088 manufacturers
- Product
- EZM 2302 1628830-21-6
- Price
- US $2.00-5.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2025-06-19