HPK1-IN-32 is a potent and specific HPK1 inhibitor (antagonist) with IC50 of 65 nM. HPK1-IN-32 may be utilized in the study of HPK1-related diseases.

Physicochemical Properties

Molecular Formula	C28H37FN8O2
Molecular Weight	536.64
Exact Mass	536.302
CAS #	2766481-17-6
PubChem CID	164889473
Appearance	White to off-white solid powder
LogP	2.4
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	8
Heavy Atom Count	39
Complexity	790
Defined Atom Stereocenter Count	1
SMILES	C1CN(C)CCC1N1C=C(OC2N=C(C3=CC(C)=C(C(NCCN4CC[C@@H](F)C4)=O)C(C)=C3)C=NC=2N)C=N1
InChi Key	IGTYEXMPMYGLTR-OAQYLSRUSA-N
InChi Code	InChI=1S/C28H37FN8O2/c1-18-12-20(13-19(2)25(18)27(38)31-7-11-36-10-4-21(29)16-36)24-15-32-26(30)28(34-24)39-23-14-33-37(17-23)22-5-8-35(3)9-6-22/h12-15,17,21-22H,4-11,16H2,1-3H3,(H2,30,32)(H,31,38)/t21-/m1/s1
Chemical Name	4-[5-amino-6-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]oxypyrazin-2-yl]-N-[2-[(3R)-3-fluoropyrrolidin-1-yl]ethyl]-2,6-dimethylbenzamide
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	HPK1
ln Vitro	With an IC50 of 65 nM, HPK1-IN-32 (Example A34, 0-2 μM, 2 h) suppresses pSLP76 activity in Jurkat cells[1].
References	[1]. 3-[(1h-pyrazol-4-yl)oxy]pyrazin-2-amine compounds as hpk1 inhibitor and use thereof. Patent. WO2022068848.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (93.17 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (4.66 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.66 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 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	1.8634 mL	9.3172 mL	18.6345 mL
	5 mM	0.3727 mL	1.8634 mL	3.7269 mL
	10 mM	0.1863 mL	0.9317 mL	1.8634 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.