Src Inhibitor 3 is a potent, orally bioactive c-terminal Src kinase (CSK) with IC50s of less than 3 nM and 4 nM in CSK HTRF and Caliper assays, respectively. Src Inhibitor 3 has the ability to enhance T cell proliferation/growth induced by T cell receptor signaling.

Physicochemical Properties

Molecular Formula	C34H32CLFN8O4
Molecular Weight	671.12
Exact Mass	670.221
CAS #	2380027-49-4
PubChem CID	139600340
Appearance	Light yellow to yellow solid powder
Density	1.4±0.1 g/cm3
Index of Refraction	1.686
LogP	2.84
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	8
Heavy Atom Count	48
Complexity	1240
Defined Atom Stereocenter Count	0
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

Targets	IC50: <3 nM (c-terminal Src kinase in CSK HTRF assay), 4 nM (c-terminal Src kinase in Caliper assay)[1]
ln Vivo	It has been demonstrated that Src Inhibitor 3 increases T cell activation in response to antigenic stimulation and decreases inhibitory LCK phosphorylation in vivo following oral treatment [1].
References	[1]. Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase. ACS Med Chem Lett. 2019 Sep 25;10(10):1486-1491.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (149.00 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (3.73 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.10 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 20.8 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	1.4900 mL	7.4502 mL	14.9005 mL
	5 mM	0.2980 mL	1.4900 mL	2.9801 mL
	10 mM	0.1490 mL	0.7450 mL	1.4900 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.