AZD-CO-Ph-PEG4-Ph-CO-AZD is a bis-β-lactam linker that can be used for antibody-siRNA conjugation synthesis.

Physicochemical Properties

Molecular Weight	496.51
Exact Mass	496.184
CAS #	2569143-72-0
PubChem CID	155422058
Appearance	White to off-white solid powder
LogP	1.2
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	13
Heavy Atom Count	36
Complexity	710
Defined Atom Stereocenter Count	0
InChi Key	UTXXKKZMYZBDCT-UHFFFAOYSA-N
InChi Code	InChI=1S/C26H28N2O8/c29-23-9-11-27(23)25(31)19-1-5-21(6-2-19)35-17-15-33-13-14-34-16-18-36-22-7-3-20(4-8-22)26(32)28-12-10-24(28)30/h1-8H,9-18H2
Chemical Name	1-[4-[2-[2-[2-[4-(2-oxoazetidine-1-carbonyl)phenoxy]ethoxy]ethoxy]ethoxy]benzoyl]azetidin-2-one
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]. Generation and validation of structurally defined antibody-siRNA conjugates. Nucleic Acids Res. 2020 Jun 4;48(10):5281-5293.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (100.70 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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	2.0141 mL	10.0703 mL	20.1406 mL
	5 mM	0.4028 mL	2.0141 mL	4.0281 mL
	10 mM	0.2014 mL	1.0070 mL	2.0141 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.