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LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
5 mg | $79 | In Stock | |
10 mg | Inquiry | In Stock | |
50 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $88 | In Stock |
Description | LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity. |
Targets&IC50 | PRMT5:(ki)6 nM, PRMT5:22 nM, MEP50:(ki)6 nM, MEP50:22 nM |
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, and a Kd of 6 nM for the PRMT5:MEP50 complex in vitro; LLY-283 inhibits A375 cell proliferation with an IC50 of 46 nM[1]. |
In vivo | LLY-283 administered orally at a dose of 20 mg/kg daily significantly inhibits tumor growth in A375 cell-bearing mice over a 28-day treatment period[1]. |
Molecular Weight | 342.35 |
Formula | C17H18N4O4 |
Cas No. | 2040291-27-6 |
Smiles | [H][C@@]1(O[C@H]([C@H](O)[C@@H]1O)n1ccc2c(N)ncnc12)[C@H](O)c1ccccc1 |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 3.57 mg/mL (10.43 mM), Sonication and heating to 60℃ are recommended. DMSO: 112.5 mg/mL (328.6 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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