Ro 08-2750 - CAS:37854-59-4

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Ro 08-2750

目录号 : KM3943 CAS No. : 37854-59-4 纯度 : 95%

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 p75^NTR 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。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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生物活性

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 inhibits NGF binding to p75 selectively over TRKA. Ro 08-2750 is a selective _{MSI RNA-binding} activity inhibitor, with an IC₅₀ of 2.7 μM.

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 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.