PeptideDB

PRO-905 2762209-68-5

PRO-905 2762209-68-5

CAS No.: 2762209-68-5

Pro-905 is a phosphite peptide with anti-tumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguano
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This product is for research use only, not for human use. We do not sell to patients.

Pro-905 is a phosphite peptide with anti-tumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to tumors. Pro-905 can effectively prevent the binding of purine residue substrates to nucleic acids and inhibit colony formation of human malignant peripheral nerve sheath tumor (MPNST) cells. Pro-905 inhibits the incorporation of purine residues into nucleic acids and prevents cell growth. Pro-905 suppresses the growth of MPNST and enhances the anti-tumor effect of JHU395.

Physicochemical Properties


Molecular Formula C22H29N6O8PS
Molecular Weight 568.54
CAS # 2762209-68-5
Appearance Typically exists as solid at room temperature
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro Pro-905 (10 µM, 120 h) and JHU395 (1 µM, 120 h) together prevent the growth of JH-2-002 cells and the incorporation of guanine into freshly generated DNA and RNA [1]. Pro-905 (10 µM, 120 h) and JHU395 (1 µM, 120 h) together have the ability to prevent sNF96.2 and JH-2-002 human MPNST cells from colonizing [1]. In sNF96.2 cells, 3H-hypoxanthine's purine-dependent binding to DNA and RNA is inhibited by Pro-905 (10 µM, 6 h) [1].
ln Vivo In an NSG mouse model harboring human MPNST PDX JH-2-031, Pro-905 (20 mg/kg, i.p., given five days a week for four weeks) inhibited the formation of tumors [1]. In the B6 flank MPNST mouse model, Pro-905 (10 mg/kg, intraperitoneal injection, given five days a week) along with JHU395 (1.2 mg/kg, po) reduced tumor nucleotide metabolism and prevented MPNST development [1].
Cell Assay Cell Proliferation Assay[1]
Cell Types: sNF96.2 and JH-2-002 human MPNST cells
Tested Concentrations: 10 µM(in combination with JHU395(HY-124778)(1µM))
Incubation Duration: 120 h
Experimental Results: Inhibited cell proliferation with effects on nucleic acid and induced DNA damage(γH2AX).
Animal Protocol Animal/Disease Models: B6 mice with flank MPNST[1]
Doses: 10 mg/kg (in combination with JHU3955 (1.2 mg/kg, po))
Route of Administration: intraperitoneal (ip)injection
Experimental Results: Prevented growth of established tumors to a greater extent. Induced tumors Dramatically decrease, mean percent proliferation, JHU395 0.82%, Pro-905 1.25%, combination 0.18%.

Animal/Disease Models: Nod scid gamma (NSG) mice with JH-2-031 MPNST [1]
Doses: 20 mg/kg
Route of Administration: intraperitoneal (ip)injection
Experimental Results: Caused animal body weights remained within 10% of starting weights over two weeks of dosing.
References [1]. Lemberg KM,et al. Pro-905, a novel purine antimetabolite, combines with glutamine amidotransferase inhibition to suppress growth of malignant peripheral nerve sheath tumor. Mol Cancer Ther. 2023 Aug 24:MCT-23-0258.

Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7589 mL 8.7945 mL 17.5889 mL
5 mM 0.3518 mL 1.7589 mL 3.5178 mL
10 mM 0.1759 mL 0.8794 mL 1.7589 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.