Description
PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain ( K d =4.7 µM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activityIn VivoPHT-7.3 (200 mg/kg; i.p.; daily; for 20 days) exhibits cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NOD-SCID mice (mut-KRas A549 NSCLC xenografts, mut-KRas H441 NSCLC xenografts) Dosage: 200 mg/kg Administration: Intraperitoneal injection, daily, for 20 days Result: Exhibited cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft. Form:SolidIC50& Target:Cnk1 PH-domain