EPZ015666
| Code | Size | Price |
|---|
| SYN-3044-M100 | 100 mg | Enquire |
Quantity:
| SYN-3044-M001 | 1 mg | £104.00 |
Quantity:
| SYN-3044-M005 | 5 mg | £186.00 |
Quantity:
| SYN-3044-M010 | 10 mg | £303.00 |
Quantity:
| SYN-3044-M050 | 50 mg | £889.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Storage:
+4°C
Documents
Further Information
Alternate Names/Synonyms:
GSK3235025; YQ36286; (S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
Appearance:
Solid.
CAS:
1616391-65-1
EClass:
32160000
Form (Short):
liquid
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
InChiKey:
ZKXZLIFRWWKZRY-KRWDZBQOSA-N
Long Description:
Chemical. CAS: 1616391-65-1. Formula: C20H25N5O3. MW: 383.4. Protein arginine methyltransferase-5 (PRMT5) is reported to have a role in diverse cellular processes, including tumorigenesis and its overexpression is observed in cell lines and primary patient samples derived from lymphomas, particularly mantle cell lymphoma (MCL). EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity in biochemical assays with an IC50 of 22nM 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. 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.
Molecular Formula:
C20H25N5O3
Molecular Weight:
383.4
Package Type:
Plastic Vial
Product Description:
Protein arginine methyltransferase-5 (PRMT5) is reported to have a role in diverse cellular processes, including tumorigenesis and its overexpression is observed in cell lines and primary patient samples derived from lymphomas, particularly mantle cell lymphoma (MCL). EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity in biochemical assays with an IC50 of 22nM 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. 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.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models: E. Chan-Penebre, et al.; Nat. Chem. Biol. 11, 432 (2015) | Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor: N. Rioux, et al.; Xenobiotica 46, 268 (2016)
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