LLY-283 Datasheet DC Chemicals
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Cat.No DC21240
Name LLY-283

Chemical Properties

CAS 2040291-27-6
Formula C17H18N4O4
MW 342.36
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description CAS NO.:2040291-27-6
Product Name:(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol
Synonyms:LLY283
EINEC:
Molecular Formula:C17H18N4O4
Molecular Weight:342.36
Target: IC50: 22 nM (PRMT5:MEP50)[1] Ki: 6 nM (PRMT5:MEP50)[1]
In Vivo LLY-283 (20 mg/kg; p.o., QD (once a day)) causes a significant inhibition on tumor growth in mice bearing A375 cells after treatment for 28 days[1].
In Vitro LLY-283 is a potent, oral and selective arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM in vitro and 25 nM in cells, as well as a Kd of 6 nM for PRMT5:MEP50 complex in vitro; LLY-283 inhibits the proliferation of A375 cell with an IC50 of 46 nM[1].
Kinase Assay
Cell Assay
Animal Administration

References

[1]. Zahid Q. Bonday, et al. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med. Chem. Lett., 2018, 9 (7), pp 612-617
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