| Size | Price | Stock | Qty |
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| Targets |
RH1's primary target is DNA. It is a prodrug that is enzymatically activated by NQO1, which is often overexpressed in solid tumors. The activated form generates DNA-alkylating species that crosslink DNA, leading to cell death.
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| ln Vitro |
RH1 (50 and 100 nM) treatment of NQ16 cells for 60 and 120 min increased the amount of cross-linked DNA significantly (p < 0.05). NQ16 cells undergo apoptosis when exposed to RH1 in a concentration- and time-dependent manner [1].
In vitro, RH1 demonstrates profound anti-cancer activity. It exhibits a dose-dependent biphasic effect, inducing apoptosis at higher doses and senescence at lower doses. It is a potent bioreductive agent against various cancer cell lines. |
| ln Vivo |
RH1 demonstrated dose-dependent anticancer efficacy against NQ16 tumors cultured in animals lacking the heart. As early as five days following the conclusion of the treatment period, NQ16 tumor-bearing mice treated with RH1 (0.4 mg/kg and 0.2 mg/kg) showed a substantial reduction in tumor volume between the treatment and control groups. Both treated and control mice showed a considerable reduction in tumor volume when given low-dose RH1 (0.1 mg/kg) [2].
In vivo, RH1 has been used in trials studying the treatment of advanced solid tumors and Non-Hodgkin's Lymphoma. It is well-tolerated with predictable and manageable toxicity in phase trials. |
| Enzyme Assay |
The cell-free assay for RH1 involves incubating the compound with recombinant NQO1 enzyme and NADPH. The reduction of RH1 is monitored spectrophotometrically. The generation of reactive intermediates can be assessed by their ability to alkylate a thiol-containing compound like glutathione.
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| Cell Assay |
For cellular assays, cancer cell lines with varying NQO1 expression levels are used. Cells are treated with RH1 under both normoxic and hypoxic conditions. Cell viability is measured using assays like MTT or clonogenic survival. DNA damage can be assessed by comet assay or γ-H2AX foci formation.
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| Animal Protocol |
In animal models, RH1 is typically administered intravenously. In xenograft models, tumor growth inhibition is measured following treatment. Toxicity is monitored by assessing body weight and clinical signs.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic parameters for RH1 are not detailed in the search results. As a small molecule prodrug, its properties are designed for activation in the tumor microenvironment.
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| Toxicity/Toxicokinetics |
In phase trials, RH1 was well tolerated with predictable and manageable toxicity. The active alkylating species is generated specifically in tumor cells, which may contribute to a favorable toxicity profile compared to systemic alkylating agents.
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| References |
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| Additional Infomation |
RH-1 has been used in trials investigating the treatment of advanced solid tumors and non-Hodgkin's lymphoma.
RH1 has been evaluated in clinical trials for the treatment of advanced solid tumors and Non-Hodgkin's Lymphoma. Its development leverages the overexpression of NQO1 in many cancers to achieve tumor-selective activation. Its status as an approved drug is not indicated in the search results. |
| Molecular Formula |
C12H14N2O3
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|---|---|
| Molecular Weight |
234.25
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| Exact Mass |
234.1
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| CAS # |
221635-42-3
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| PubChem CID |
394347
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| Appearance |
Brown to red solid powder
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| LogP |
0.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
482
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JKDLOGLNPDVUCX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H14N2O3/c1-7-9(13-2-3-13)12(17)8(6-15)10(11(7)16)14-4-5-14/h15H,2-6H2,1H3
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| Chemical Name |
2,5-bis(aziridin-1-yl)-3-(hydroxymethyl)-6-methylcyclohexa-2,5-diene-1,4-dione
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| Synonyms |
NSC 697726; NSC697726; NSC697726
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2689 mL | 21.3447 mL | 42.6894 mL | |
| 5 mM | 0.8538 mL | 4.2689 mL | 8.5379 mL | |
| 10 mM | 0.4269 mL | 2.1345 mL | 4.2689 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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