bs-60254C
[Life Science]
EPZ015666 (GSK3235025) --- PRMT5 Inhibitor
DATASHEET
Formulation Powder
Storage: Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 383.44
Formula: C20 H25 N5 O3
CAS Number: 1616391-65-1
InChi Key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N
InChi: InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1
Smiles: O[C@@H](CNC(=O)C1C=C(NC2COC2)N=CN=1)CN1CCC2=CC=CC=C2C1
Purity: 98.0
Solubility: DMSO and EtOH up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Formula: C20 H25 N5 O3
CAS Number: 1616391-65-1
InChi Key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N
InChi: InChI=1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-/m0/s1
Smiles: O[C@@H](CNC(=O)C1C=C(NC2COC2)N=CN=1)CN1CCC2=CC=CC=C2C1
Purity: 98.0
Solubility: DMSO and EtOH up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
EPZ015666, also known as GSK3235025, is a potent and selective and orally active PRMT5 inhibitor with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.
Size: 2 mg solid,10 mg solid 2 mg solid,10 mg solid
Applications: Life Science()
For research use only. Not intended for diagnostic or therapeutic use.