RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC 50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.