Ro 08-2750

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ro 08-2750 是一种非肽可逆神经生长因子 (NGF) 抑制剂，可与 NGF 结合，IC50 约为 1 μM。

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.(In Vitro):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 .(In Vivo):In a myeloid leukemia model in vivo, Ro 08-2750 (13.75?mg/kg; i.p.) suppresses leukemogenesis .

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 (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.

Ro 08-2750 (13.75mg/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.

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Others

Other Targets

AhR| Androgen Receptor| Antifungal| Estrogen Receptor/ERR

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37854-59-4

270.248

C13H10N4O3

>98% (HPLC)

In Vitro:?DMSO : 4 mg/mL (14.80 mM)

Cc1cc2nc3c(nc(=O)[nH]c3=O)n(C)c2cc1C=O

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(-20℃)

With Ice Pack

≥ 2 years