Ro 08-2750

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Ro 08-2750  纯度: 95.01%

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。

Ro 08-2750

Ro 08-2750 Chemical Structure

CAS No. : 37854-59-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4608 询价
1 mg ¥1550 In-stock
5 mg ¥4650 询价
10 mg   询价  
50 mg   询价  

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Ro 08-2750 相关产品

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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 p75NTR selectively over TRKA[1]. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 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 p75NTR anymore[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[3]

Cell Line: MLL-AF9 + BM cells
Concentration: 5 μM, 10 μM
Incubation Time: 8 hours
Result: Increased apoptosis.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

270.24

Formula

C13H10N4O3

CAS 号

37854-59-4

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
溶解性数据
In Vitro: 

DMSO : 4 mg/mL (14.80 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Arkin MR, et al. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov. 2004 Apr;3(4):301-17.

    [2]. Niederhauser O, et al. NGF ligand alters NGF signaling via p75(NTR) and trkA. J Neurosci Res. 2000 Aug 1;61(3):263-72.

    [3]. Minuesa G, et al. Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia. Nat Commun. 2019 Jun 19;10(1):2691.

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