Ro 08-2750 是一种非肽和可逆的神经生长因子 (NGF) 抑制剂,与 NGF 结合,IC50 约为 1 μM。它是一种选择性 MSI RNA 结合活性抑制剂,IC50 为 2.7 μM。它选择性抑制 NGF 与 p75NTR 的结合,而不是 TRKA。
产品描述
Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 μM. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM. Ro 08-2750 inhibits NGF binding to p75NTR selectively over TRKA.
体外活性
Ro 08-2750 inhibits the survival of human AML lines and patient cells. Ro 08-2750 suppresses MSI2 RNA-binding and alters the MSI2 gene signature. Ro 08-2750 binds to the NGF dimer thereby probably inducing a change in its conformation such that NGF cannot bind to p75NTR anymore. Ro 08-2750 (5-10 μM; 8 hours) increases differentiation and apoptosis in myeloid leukemia cells. Ro 08-2750 (10 nM) fully rescues cells from undergoing NGF-induced SK-N-MC 103 cell death [2][3].
体内活性
In a myeloid leukemia model in vivo, Ro 08-2750 (13.75 mg/kg; i.p.) suppresses leukemogenesis [3].
Cas No.
37854-59-4
分子式
C13H10N4O3
分子量
270.24
储存和溶解度
DMSO:3.5 mg/mL (12.95 mM),ultrasonic and warming and heat to 80°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years