HPK1-IN-55 

HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC_{50 of <0.51 nM. HPK1-IN-55 shows excellent kinase selectivity (>637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects^[1].}

HPK1-IN-55 (0.5-10000 nM, 5 h) demonstrates enzymatic inhibition (IC_{50 <0.51 nM) and cellular potency (EC50 = 43.3 nM) in human PBMCs ^[1].
HPK1-IN-55 (0.001-100 nM) stimulates IL-2 and IFN-γ release with EC50 values of 38.8 and 49.2 nM, respectively in purified human pan T cells^[1].
HPK1-IN-55 (0.00457-10 μM, 72 h) increases T cell proliferation at low, intermediate and high concentrations in human pan T cells^[1].}

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) exerts good antitumor effects as a monotherapy, which shows an additive effect in the CT26 model and a synergistic effect in the MC38 model when combined with anti-PD-1^[1].
HPK1-IN-55 (1 mg/kg, i.v., 2 mg/kg, p.o.) exhibits moderate clearance (Clp = 11.41mL/min/kg) as well as good oral exposure (DNAUC(0−24h) = 560.5 h•ng/mL) and bioavailability (F % = 42.0) in monkeys^[1].
HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) exhibits good target engagement in the CT26 model^[1].
In Vivo Pharmacokinetics of HPK1-IN-55 .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

554.64

C₃₀H₃₄N₈O₃

3048537-58-9

COC1=CC(NC2=CC=C3C4(N(CC3=N2)C)CCN(CC4)C5COC5)=C(N=C1C6=C(C7=CC=C6)N=CN7C)C(N)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Peng J, et.al. Discovery of Pyridine-2-Carboxamides Derivatives as Potent and Selective HPK1 Inhibitors for the Treatment of Cancer. J Med Chem. 2024 Dec 12;67(23):21520-21544.  [Content Brief]