LLY-284

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

LLY-284
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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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Product Promise

Promise
Molecular Weight (MW)342.36
Molecular FormulaC17H18N4O4
CAS No.2226515-75-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility In VitroDMSO: > 50 mg/mL
Water: N/A
Ethanol: N/A
Solubility In VivoN/A
SynonymsO[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
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.9209 mL14.6045 mL29.2090 mL58.4180 mL
5mM0.5842 mL2.9209 mL5.8418 mL11.6836 mL
10mM0.2921 mL1.4605 mL2.9209 mL5.8418 mL
20mM0.1460 mL0.7302 mL1.4605 mL2.9209 mL
Quality Control Documentation
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)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
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.