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LLY-283 

Cat. No.: HY-107777
Handling Instructions

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.

For research use only. We do not sell to patients.

LLY-283 Chemical Structure

LLY-283 Chemical Structure

CAS No. : 2040291-27-6

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target

IC50: 22 nM (PRMT5:MEP50)[1]
Ki: 6 nM (PRMT5:MEP50)[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].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9210 mL 14.6049 mL 29.2099 mL
5 mM 0.5842 mL 2.9210 mL 5.8420 mL
10 mM 0.2921 mL 1.4605 mL 2.9210 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

342.35

Formula

C₁₇H₁₈N₄O₄

CAS No.

2040291-27-6

SMILES

O[[email protected]]1[[email protected]@H](O[[email protected]@]([[email protected]@H](C2=CC=CC=C2)O)([H])[[email protected]]1O)N3C4=NC=NC(N)=C4C=C3

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
LLY-283
Cat. No.:
HY-107777
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LLY-283

Cat. No.: HY-107777