Onalespib (lactate)

Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an K_d value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC)^[1][2][3][4]. In Vitro: Onalespib lactate (0-0.4 µM; 72 h, 48 h) inhibits the proliferation, survival and migration of glioma cells^[2].
Onalespib lactate (0-0.4 µM; 48 h) decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner^[2]. In Vivo: Onalespib lactate (30 mg/kg; i.v.; once) crosses the blood-brain barrier (BBB) and causes sustained inhibition of HSP90 in 6-week-old ICR mice^[2].
Onalespib lactate (0.5 µM; from 5 to 10 days post-transplant) and TMZ (10 µM) reduce tumor growth and extend survival in zebrafish embryos^[2].
Onalespib lactate (5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts; i.p.; daily for 3 days) shows anti-tumor activity in HCT116 and A431 xenografts^[3].