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。
| 生物活性 | Ro 08-2750 is a non-peptide and reversiblenerve growth factor (NGF)inhibitor which binds to NGF, and with anIC50of ~ 1 μM. Ro 08-2750 inhibits NGF binding to p75NTRselectively overTRKA[1]. Ro 08-2750 is a selectiveMSI RNA-bindingactivity inhibitor, with anIC50of 2.7 μM[3]. |
| IC50& Target | IC50: ~1 μM (NGF)[1], 2.7 μM (MSI RNA-binding)[3] |
体外研究
(In Vitro) | Ro 08-2750 binds to the NGF dimer thereby probably inducing a change in its conformation such that NGF cannot bind to p75NTRanymore[2].
Ro 08-2750 (10 nM) completely rescues cells from undergoing NGF-induced SK-N-MC 103 cells death[2].
Ro 08-2750 (5-10 μM; 8 hours) increases differentiation and apoptosis in myeloid leukemia cells[3].
Ro 08-2750 inhibits survival of human AML lines and patient cells[3].
Ro 08-2750 inhibits MSI2 RNA-binding and alters MSI2 gene signature[3].
Apoptosis Analysis[3] | Cell Line: | MLL-AF9 + BM cells | | Concentration: | 5 μM, 10 μM | | Incubation Time: | 8 hours | | Result: | Increased apoptosis. |
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体内研究
(In Vivo) | Ro 08-2750 (13.75 mg/kg; i.p.) inhibits leukemogenesis in a myeloid leukemia model in vivo[3].
| Animal Model: | C57BL/6 wild type mice (10-12-weeks-old), MLL-AF9 murine leukemia model[3] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 4 mg/mL(14.80 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL | | 5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL | | 10 mM | 0.3700 mL | 1.8502 mL | 3.7004 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
