ALV1 efficiently induces Ikaros and Helios degradation without unexpected off-target effects. ALV1 binds CRBN with IC50 of 0.55 µM. ALV1 degrades cells stably expressing IKZF1Δ and IKZF2Δ GFP fusions with DC50 of 2.5 and 10.3 nM, respectively.

Physicochemical Properties

Molecular Formula	C25H23CLN4O5
Molecular Weight	494.93
Exact Mass	494.135
CAS #	2438124-79-7
PubChem CID	146628546
Appearance	Light yellow to green yellow solid powder
LogP	2.5
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	7
Heavy Atom Count	35
Complexity	922
Defined Atom Stereocenter Count	0
SMILES	C1(CCC(NC2=CC=C(C)C(Cl)=C2)=O)=CC=CC(NC2=CC(=O)N(C3CCC(=O)NC3=O)C2=O)=C1
InChi Key	YDYSAFPHVGVORZ-UHFFFAOYSA-N
InChi Code	InChI=1S/C25H23ClN4O5/c1-14-5-7-17(12-18(14)26)28-21(31)9-6-15-3-2-4-16(11-15)27-19-13-23(33)30(25(19)35)20-8-10-22(32)29-24(20)34/h2-5,7,11-13,20,27H,6,8-10H2,1H3,(H,28,31)(H,29,32,34)
Chemical Name	N-(3-chloro-4-methylphenyl)-3-[3-[[1-(2,6-dioxopiperidin-3-yl)-2,5-dioxopyrrol-3-yl]amino]phenyl]propanamide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 2021 Jun;17(6):711-717.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~101.02 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (5.05 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0205 mL	10.1024 mL	20.2049 mL
	5 mM	0.4041 mL	2.0205 mL	4.0410 mL
	10 mM	0.2020 mL	1.0102 mL	2.0205 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.