ALV2

ALV2 is a potent and selective Helios degrader. ALV2 binds CRBN, with an IC50 of 0.57 μM. Helios is the zinc-finger transcription factor that can maintain a stable Treg cell phenotype in the inflammatory tumor microenvironment.

Product information

CAS Number: 2438124-95-7

Molecular Weight: 523.97

Formula: C26H26ClN5O5

Chemical Name: N-(3-chloro-4-methylphenyl)-N'-[1-[3-[[1-(2, 6-dioxo-3-piperidinyl)-2, 5-dihydro-2, 5-dioxo-1H-pyrrol-3-yl]amino]phenyl]-1-methylethyl]-

Smiles: CC1=CC=C(C=C1Cl)NC(=O)NC(C)(C)C1=CC(=CC=C1)NC1=CC(=O)N(C2CCC(=O)NC2=O)C1=O

InChiKey: YKFHBIMJVFQOQL-UHFFFAOYSA-N

InChi: InChI=1S/C26H26ClN5O5/c1-14-7-8-17(12-18(14)27)29-25(37)31-26(2,3)15-5-4-6-16(11-15)28-19-13-22(34)32(24(19)36)20-9-10-21(33)30-23(20)35/h4-8,11-13,20,28H,9-10H2,1-3H3,(H2,29,31,37)(H,30,33,35)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

ALV2 (10 nM-100 μM) induces CRBN-Helios dimerization in the TR-FRET assay. ALV2 (0.1-10 μM) preferentially promotes Helios degradation in Jurkat cells. ALV2 (1 μM; pretreated for 18 h) promotes IL-2 secretion in Jurkat cells.

In Vivo:

ALV2 (100 mg/kg; i.p. twice daily for 7 days) induces selective Helios degradation in vivo.

References:

1. Wang ES, et, al. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.

Products are for research use only. Not for human use.