HEI3090 is a P2X7R activator. HEI3090 stimulates dendritic P2X7R-expressing cells to produce IL-18, which in turn promotes the production of IFN-γ by natural killer cells and CD4 T cells in tumors, triggering a lasting anti-tumor response. HEI3090 can be used to enhance the efficacy of αPD-1 therapy in non-small cell lung cancer (NSCLC).

Physicochemical Properties

Molecular Formula	C18H15CL3N4O3
Molecular Weight	441.70
CAS #	2377167-56-9
Appearance	White to off-white solid powder
SMILES	N1(C(NC2=CC=C(Cl)N=C2)=O)C(=O)CC[C@H]1C(NCC1=CC=C(Cl)C=C1Cl)=O
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	P2X7 Receptor
References	[1]. Douguet L, et al. A small-molecule P2RX7 activator promotes anti-tumor immune responses and sensitizes lung tumor to immunotherapy. Nat Commun. 2021 Jan 28;12(1):653.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~113.20 mM; with ultrasonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 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 the 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2640 mL	11.3199 mL	22.6398 mL
	5 mM	0.4528 mL	2.2640 mL	4.5280 mL
	10 mM	0.2264 mL	1.1320 mL	2.2640 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.