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| Cas No.: | 2040291-27-6 |
| Chemical 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 |
| SMILES: | O1[C@H]([C@H](O)C2=CC=CC=C2)[C@@H](O)[C@@H](O)[C@@H]1N1C2C(C=C1)=C(N)N=CN=2 |
| Formula: | C17H18N4O4 |
| M.Wt: | 342.36 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity. |
| 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]. |
| 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 |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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