Ro 08-2750

• CAS: 37854-59-4
• Catalog Number: ACM37854594
• Category: Inhibitors
• Molecular Weight: 270.25
• Molecular Formula: C13H10N4O3
• Description: Ro 08-2750 is a potent and selective Nerve growth factor (NGF) inhibitor that binds the NGF dimer (KD ~ 1 μM). NGF has potential effects on matrix turnover activity and influences the catabolic/anabolic balance of IVD cells in an adverse way that may potentiate IVD degeneration. Anti-NGF treatment might be beneficial to ameliorate progressive tissue breakdown in IVD degeneration and may lead to pain relief.
• Synonyms: Ro 08-2750; Ro08-2750; Ro-08-2750; Ro 082750; Ro -082750; Ro082750
• IUPAC Name: 2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde
• Canonical SMILES: O=CC1=C(C)C=C2N=C3C(NC(N=C3N(C)C2=C1)=O)=O
• InChI: InChI=1S/C13H10N4O3/c1-6-3-8-9(4-7(6)5-18)17(2)11-10(14-8)12(19)16-13(20)15-11/h3-5H,1-2H3,(H,16,19,20)
• InChI Key: JDEMVNYMYPJJIM-UHFFFAOYSA-N
• Solubility: Soluble in DMSO, not in water
• Appearance: Orange to red solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: 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.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 57.78; H, 3.73; N, 20.73; O, 17.76
• Exact Mass: 270.07529
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: Ro 08-2750, a small non-peptide molecule, was found to bind to NGF and dimer itself, which induces a concentration-dependent and time-dependent conformational change of NGF that depending on the cell types, cell growth conditions or combination form with receptors. This study found the decreased levels of β-catenin mRNA in the three cells induced by 100 ng/ml NGF can be up-regulated significantly by Ro 08-2750, K252a and LM11A-31.; Reference: Oncotarget. 2016 Dec 6; 7(49): 81026-81048. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5348374/
• In Vivo Activity: Using healthy mice, this study also reported no changes in liver enzymes 24 h after Ro treatment (Supplementary Fig. 8g). Although there was no change in leukemia latency in this very aggressive model, disease progression was assessed in both treated and control groups when control mice and treated mice succumbed to disease (day 19 post-transplantation). The treated group exhibited a significant reduction in spleen weights (Fig. 6e), white blood cell counts (Fig. 6f) and c-MYC levels compared with the control group (Fig. 6g). These data support the concept that targeting MSI in vivo could have therapeutic efficacy in AML.; Reference: Nat Commun. 2019; 10: 2691. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6584500/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).