LLY-284 | CAS 2226515-75-7

LLY-284

This product is for research use only, not for human use. We do not sell to patients.

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Cat #: V3139 CAS #: 2226515-75-7 Purity ≥ 98%

Description: LLY-284 (LLY284) is a negative control and tool compound for LLY-283. It is a diastereomer of LLY-283 but was much less active. LLY-283 (LLY283) is the first-in-class and selective SAM-competitive inhibitor of PRMT5 (protein arginine methyltransferase 5) with antitumor activity. LLY-283 inhibited PRMT5 enzymatic activity in vitro and in cells with IC50 values of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 also showed antitumor activity in mouse xenografts when dosed orally and can serve as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. PRMT5 is ubiquitously expressed in most tissues and its expression has been shown to be elevated in several cancers including breast cancer, gastric cancer, glioblastoma, and lymphoma. PRMTs binds to the lysine or arginine residues of substrate proteins via the substrate binding groove and SAM via the cofactor binding site.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	342.36
Molecular Formula	C17H18N4O4
CAS No.	2226515-75-7
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: > 50 mg/mL
	Water: N/A
	Ethanol: N/A
Solubility In Vivo	N/A
Synonyms	O[C@H]1[C@H](N2C=CC3=C(N)N=CN=C32)O[C@H]([C@@H](O)C4=CC=CC=C4)[C@H]1O

Related Biological Data

ACS Med. Chem. Lett. (2018) DOI: 10.1021/acsmedchemlett.8b00014

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.9209 mL	14.6045 mL	29.2090 mL	58.4180 mL
5mM	0.5842 mL	2.9209 mL	5.8418 mL	11.6836 mL
10mM	0.2921 mL	1.4605 mL	2.9209 mL	5.8418 mL
20mM	0.1460 mL	0.7302 mL	1.4605 mL	2.9209 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.