Ro 08-2750
目录号 : GC17622
Ro 08-2750是一种竞争性Musashi (MSI)-RNA相互作用抑制剂，IC50值为2.7±0.4µM。
Cas No.:37854-59-4
Sample solution is provided at 25 µL, 10mM.
Ro 08-2750 is a competitive inhibitor of Musashi (MSI)–RNA interactions, with an IC50 value of 2.7±0.4µM [1]. Ro 08-2750-mediated inhibition of MSI can reduce aldosterone production, with an IC50 value of 1.50± 0.154µM[2]. Ro 08-2750 has been widely applied in disease models to regulate the expression and activity of nerve growth factors[3].
In vitro, Ro 08-2750 treatment for 96 hours significantly inhibited the viability of MDA-MB-468 cells, SUM149PT cells, UIVC-IDC-2 cells and UIVC-IDC-4 cells with IC50 values of 6.3µM, 12.8µM, 12.8µM, and 14µM, respectively[4]. Treatment with 10μM Ro 08-2750 for 7 days significantly inhibited the expression of osteogenic-related genes and protein markers in dental pulp stem cells[5]. The 2nM Ro 08-2750 treatment for 24 hours on MDA-MB-231 cells significantly inhibited the expression of p75NTR protein[6].
In vivo, Ro 08-2750 treatment via intraperitoneal injection (13.75mg/kg) once every two days for two consecutive weeks significantly inhibited the growth of xenograft tumors in the cervical cancer mouse model and significantly increased the levels of p-LATS1 and p-YAP proteins in the tumor tissues[7]. By intraperitoneal injection at a dose of 7.0mg/kg twice a week for 21 days, Ro 08-2750 significantly inhibited the tumor burden in a chronic lymphocytic leukemia (CLL) mouse model[8].
References:
[1] Minuesa G, Albanese S K, Xie W, et al. Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia[J]. Nature communications, 2019, 10(1): 2691.
[2] Walters K, Sajek M P, Murphy E, et al. Small-molecule Ro-08-2750 interacts with many RNA-binding proteins and elicits MUSASHI2-independent phenotypes[J]. Rna, 2023, 29(10): 1458-1470.
[3] Kao T H, Peng Y J, Salter D M, et al. Nerve growth factor increases MMP9 activity in annulus fibrosus cells by upregulating lipocalin 2 expression[J]. European Spine Journal, 2015, 24(9): 1959-1968.
[4] Brücksken K A, Sicking M, Korsching E, et al. Musashi inhibitor Ro 08–2750 attenuates triple-negative breast cancer cell proliferation and migration and acts as a novel chemo-and radiosensitizer[J]. Biomedicine & pharmacotherapy, 2025, 186: 118002.
[5] Cheng C, Tang S, Cui S, et al. Nerve growth factor promote osteogenic differentiation of dental pulp stem cells through MEK/ERK signalling pathways[J]. Journal of Cellular and Molecular Medicine, 2024, 28(4): e18143.
[6] Chakravarthy R, Mnich K, Gorman A M. Nerve growth factor (NGF)-mediated regulation of p75NTR expression contributes to chemotherapeutic resistance in triple negative breast cancer cells[J]. Biochemical and biophysical research communications, 2016, 478(4): 1541-1547.
[7] Wang L, Li J, Wang R, et al. NGF signaling interacts with the Hippo/YAP pathway to regulate cervical cancer progression[J]. Frontiers in oncology, 2021, 11: 688794.
[8] Palacios F, Yan X J, Ferrer G, et al. Musashi 2 influences chronic lymphocytic leukemia cell survival and growth making it a potential therapeutic target[J]. Leukemia, 2021, 35(4): 1037-1052.
Ro 08-2750是一种竞争性Musashi (MSI)-RNA相互作用抑制剂，IC50值为2.7±0.4µM[1]。Ro 08-2750通过抑制MSI功能可降低醛固酮生成，IC50值为1.50±0.154µM[2]。Ro 08-2750已广泛应用于疾病模型中调控神经生长因子的表达与活性[3]。
在体外，Ro 08-2750处理96小时能显著抑制MDA-MB-468、SUM149PT、UIVC-IDC-2和UIVC-IDC-4细胞活力，IC50值分别为6.3µM、12.8µM、12.8µM和14µM[4]。使用10μM的Ro 08-2750处理牙髓干细胞7天，可显著抑制成骨相关基因和蛋白标志物的表达[5]。用2nM的Ro 08-2750处理MDA-MB-231细胞24小时，能显著抑制p75NTR蛋白表达[6]。
在体内，Ro 08-2750通过腹腔注射（13.75mg/kg）每两天一次，连续进行两周，可显著抑制宫颈癌小鼠模型移植瘤的生长，并提高肿瘤组织中p-LATS1和p-YAP蛋白水平[7]。通过每周两次腹腔注射7.0mg/kg剂量的Ro 08-2750连续21天，能显著减轻慢性淋巴细胞白血病(CLL)小鼠模型的肿瘤负荷[8]。
| Cell experiment [1]: | |
Cell lines | MDA-MB-468 cells |
Preparation Method | MDA-MB-468 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum, 1% penicillin/streptomycin, and 20mM HEPES at 37℃, 5% CO2, and 90% humidity. 4000 MDA-MB-468 cells were seeded in 96-well plates. Subsequently, cells were treated with Ro 08-2750 at different concentrations (0.1, 1, 5, 10, 15, 20, and 25µM). After 96 hours, the supernatant was discarded, the MTT solution was added, and after 24 hours of incubation, the well plates were analyzed using a microplate reader to measure the absorbance at 570nm. |
Reaction Conditions | 0.1, 1, 5, 10, 15, 20, and 25µM; 96h |
Applications | Ro 08-2750 treatment inhibited the viability of MDA-MB-468 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | Four-week-old female BALB/c nude mice were raised under SPF (specific pathogen-free) conditions, with a temperature of 22-25℃ and humidity of 40-50%. Logarithmic growth phase cells were counted under aseptic conditions. HeLa cells (1×106) were suspended in 100μl of phosphate-buffered saline (PBS), and then injected subcutaneously into the anterior back of BALB/c nude mice. On the 10th day after tumor cell implantation (when the tumor volume reached approximately 50mm3), the tumor-bearing mice were randomly grouped. The mice were intraperitoneally injected with Ro 08-2750 at a dose of 13.75mg/kg, and the injection was administered every 2 days for a total of 2 weeks. The tumor size was measured with a vernier caliper every 2 days. |
Dosage form | 13.75mg/kg; every 2 days for 2 weeks; i.p. |
Applications | Ro 08-2750 treatment significantly inhibited tumor formation in mice without affecting body weight. |
References: | |
| Cas No. | 37854-59-4 | SDF | |
| 化学名 | 7,10-dimethyl-2,4-dioxo-2,3,4,10-tetrahydrobenzo[g]pteridine-8-carbaldehyde | ||
| Canonical SMILES | O=C1NC(N=C2N(C)C3=CC(C=O)=C(C)C=C3N=C21)=O | ||
| 分子式 | C13H10N4O3 | 分子量 | 270.24 |
| 溶解度 | DMSO : 4 mg/mL (14.80 mM; ultrasonic and warming and heat to 80°C) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL |
| 5 mM | 740.1 μL | 3.7004 mL | 7.4008 mL |
| 10 mM | 370 μL | 1.8502 mL | 3.7004 mL |
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