37854-59-4
中文名称
7,10-DIMETHYL-2,4-DIOXOBENZO[G]PTERIDINE-8-CARBALDEHYDE
英文名称
RO 08-2750
CAS
37854-59-4
分子式
C13H10N4O3
分子量
270.24
MOL 文件
37854-59-4.mol
更新日期
2024/05/23 20:39:41
37854-59-4 结构式
基本信息
中文别名
化合物 T16766化合物RO 08-2750
英文别名
RO 08-27507,10-DIMETHYL-2,4-DIOXOBENZO[G]PTERIDINE-8-CARBALDEHYDE
2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde
Benzo[g]pteridine-8-carboxaldehyde, 2,3,4,10-tetrahydro-7,10-dimethyl-2,4-dioxo-
常见问题列表
生物活性
Ro 08-2750 是一种非肽、可逆的 NGF 抑制剂，能直接结合 NGF，IC50 值为 ~ 1 µM。Ro 08-2750 能抑制 NGF 结合 p75NTR 的优于 TRKA。Ro 08-2750 是选择性的 MSI RNA 结合抑制剂，其作用的 IC50 值为 2.7 μM。靶点
IC50: ~1 µM (NGF), 2.7 μM (MSI RNA-binding)
体外研究
Ro 08-2750 binds to the NGF dimer thereby probably inducing a change in its conformation such that NGF cannot bind to p75
NTR
anymore.
Ro 08-2750 (10 nM) completely rescues cells from undergoing NGF-induced SK-N-MC 103 cells death.
Ro 08-2750 (5-10 μM; 8 hours) increases differentiation and apoptosis in myeloid leukemia cells.
Ro 08-2750 inhibits survival of human AML lines and patient cells.
Ro 08-2750 inhibits MSI2 RNA-binding and alters MSI2 gene signature.
Apoptosis Analysis
| Cell Line: | MLL-AF9 + BM cells |
| Concentration: | 5 μM, 10 μM |
| Incubation Time: | 8 hours |
| Result: | Increased apoptosis. |
体内研究
Ro 08-2750 (13.75 mg/kg; i.p.) inhibits leukemogenesis in a myeloid leukemia model in vivo.
| Animal Model: | C57BL/6 wild type mice (10-12-weeks-old), MLL-AF9 murine leukemia model |
| Dosage: | 13.75 mg/kg |
| Administration: | Intraperitoneal injection, at days 1, 4, 7, 10, and 13 (one day on, two days off drug) |
| Result: | Inhibited c-MYC levels and reduced disease burden. |