Ro 08-2750
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MedKoo CAT#: 522399

CAS#: 37854-59-4

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.


Chemical Structure

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Ro 08-2750
CAS# 37854-59-4

Theoretical Analysis

MedKoo Cat#: 522399
Name: Ro 08-2750
CAS#: 37854-59-4
Chemical Formula: C13H10N4O3
Exact Mass: 270.07529
Molecular Weight: 270.25
Elemental Analysis: C, 57.78; H, 3.73; N, 20.73; O, 17.76

Price and Availability

Size Price Availability Quantity
5.0mg USD 90.0 Ready to ship
10.0mg USD 150.0 Ready to ship
25.0mg USD 320.0 Ready to ship
50.0mg USD 550.0 Ready to ship
100.0mg USD 850.0 Ready to ship
200.0mg USD 1450.0 Ready to ship
500.0mg USD 3250.0 Ready to ship
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Synonym: Ro 08-2750; Ro08-2750; Ro-08-2750; Ro 082750; Ro -082750; Ro082750.

IUPAC/Chemical Name: 2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde

InChi Key: JDEMVNYMYPJJIM-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=CC1=C(C)C=C2N=C3C(NC(N=C3N(C)C2=C1)=O)=O

Appearance: Orange to red solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: 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.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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.
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.7 10.0

Preparing Stock Solutions

The following data is based on the product molecular weight 270.25 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Minuesa G, Albanese SK, Xie W, Kazansky Y, Worroll D, Chow A, Schurer A, Park SM, Rotsides CZ, Taggart J, Rizzi A, Naden LN, Chou T, Gourkanti S, Cappel D, Passarelli MC, Fairchild L, Adura C, Glickman JF, Schulman J, Famulare C, Patel M, Eibl JK, Ross GM, Bhattacharya S, Tan DS, Leslie CS, Beuming T, Patel DJ, Goldgur Y, Chodera JD, Kharas MG. Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia. Nat Commun. 2019 Jun 19;10(1):2691. doi: 10.1038/s41467-019-10523-3. PMID: 31217428; PMCID: PMC6584500. 2. Li B, Cai S, Zhao Y, He Q, Yu X, Cheng L, Zhang Y, Hu X, Ke M, Chen S, Zou M. Nerve growth factor modulates the tumor cells migration in ovarian cancer through the WNT/β-catenin pathway. Oncotarget. 2016 Dec 6;7(49):81026-81048. doi: 10.18632/oncotarget.13186. PMID: 27835587; PMCID: PMC5348374.
In vitro protocol: 1. Minuesa G, Albanese SK, Xie W, Kazansky Y, Worroll D, Chow A, Schurer A, Park SM, Rotsides CZ, Taggart J, Rizzi A, Naden LN, Chou T, Gourkanti S, Cappel D, Passarelli MC, Fairchild L, Adura C, Glickman JF, Schulman J, Famulare C, Patel M, Eibl JK, Ross GM, Bhattacharya S, Tan DS, Leslie CS, Beuming T, Patel DJ, Goldgur Y, Chodera JD, Kharas MG. Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia. Nat Commun. 2019 Jun 19;10(1):2691. doi: 10.1038/s41467-019-10523-3. PMID: 31217428; PMCID: PMC6584500. 2. Li B, Cai S, Zhao Y, He Q, Yu X, Cheng L, Zhang Y, Hu X, Ke M, Chen S, Zou M. Nerve growth factor modulates the tumor cells migration in ovarian cancer through the WNT/β-catenin pathway. Oncotarget. 2016 Dec 6;7(49):81026-81048. doi: 10.18632/oncotarget.13186. PMID: 27835587; PMCID: PMC5348374.
In vivo protocol: 1. Minuesa G, Albanese SK, Xie W, Kazansky Y, Worroll D, Chow A, Schurer A, Park SM, Rotsides CZ, Taggart J, Rizzi A, Naden LN, Chou T, Gourkanti S, Cappel D, Passarelli MC, Fairchild L, Adura C, Glickman JF, Schulman J, Famulare C, Patel M, Eibl JK, Ross GM, Bhattacharya S, Tan DS, Leslie CS, Beuming T, Patel DJ, Goldgur Y, Chodera JD, Kharas MG. Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia. Nat Commun. 2019 Jun 19;10(1):2691. doi: 10.1038/s41467-019-10523-3. PMID: 31217428; PMCID: PMC6584500.

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1: Kao TH, Peng YJ, Salter DM, Lee HS. Nerve growth factor increases MMP9 activity in annulus fibrosus cells by upregulating lipocalin 2 expression. Eur Spine J. 2015 Sep;24(9):1959-68. doi: 10.1007/s00586-014-3675-2. Epub 2014 Nov 21. PubMed PMID: 25412834.

2: Kao TH, Peng YJ, Tsou HK, Salter DM, Lee HS. Nerve growth factor promotes expression of novel genes in intervertebral disc cells that regulate tissue degradation: Laboratory investigation. J Neurosurg Spine. 2014 Oct;21(4):653-61. doi: 10.3171/2014.6.SPINE13756. Epub 2014 Jul 25. PubMed PMID: 25062286.

3: Eibl JK, Strasser BC, Ross GM. Identification of novel pyrazoloquinazolinecarboxilate analogues to inhibit nerve growth factor in vitro. Eur J Pharmacol. 2013 May 15;708(1-3):30-7. doi: 10.1016/j.ejphar.2013.03.029. Epub 2013 Mar 22. PubMed PMID: 23528360.

4: Niederhauser O, Mangold M, Schubenel R, Kusznir EA, Schmidt D, Hertel C. NGF ligand alters NGF signaling via p75(NTR) and trkA. J Neurosci Res. 2000 Aug 1;61(3):263-72. PubMed PMID: 10900073.