Gemcitabine-O-Si(di-iso)-O-Mc is an acid-cleavable ADC (antibody-drug conjugate) linker used for ADC synthesis with potent antitumor activity. As a drug-linker conjugate, it employs Gemcitabine linked via the ADC linker.

Physicochemical Properties

Molecular Formula	C??H??F?N?O?SI
Molecular Weight	558.65
Appearance	Typically exists as Off-white to light yellow solids at room temperature
Synonyms	GemcitabineOSi(diiso)OMc Gemcitabine O Si(di iso) O Mc
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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage.(2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
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

ln Vitro	Therapeutic monoclonal antibodies (mAbs) are conjugated to strong toxins via antibody drug conjugates (ADCs), which cleave the linker inside target cells but remain stable in the systemic circulation [1].
References	[1]. A versatile acid-labile linker for antibody–drug conjugate. MedChemComm, Issue 9, 2014.
Additional Infomation	Antibody drug conjugates (ADC) couple therapeutic monoclonal antibodies (mAb) with potent toxins through a linker that is stable within systemic circulation, but cleaves within the target cells. In this report, silyl ether chemistry was used to couple the mAb trastuzumab with the chemotherapeutic, gemcitabine, to demonstrate the use of silyl ethers as a potential linker for ADCs.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (4.48 mM) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.7900 mL	8.9501 mL	17.9003 mL
	5 mM	0.3580 mL	1.7900 mL	3.5801 mL
	10 mM	0.1790 mL	0.8950 mL	1.7900 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.