| Size | Price | Stock | Qty |
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| 10mg |
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| ln Vitro |
The mechanism of action of CNDAC is distinct; upon entering DNA, it causes single-strand breaks (SSBs), which are subsequently transformed into double-strand breaks (DSBs) during the second S phase of cell division [1]. CNDAC (0-100 μM; 3 days) prevents HL-60 and THP-1 cells from swelling [2]. A number of cells, including Rad51D and XRCC3, are susceptible to CNDAC (0–1 μM; 24 h) [1]. After a delayed S phase, CNDAC (6 μM; 48 h) causes cell cycle arrest in HCT116 cells during the G2 phase [3]. -10 μM; 3–6 days) to cause HL-60 and THP-1 cells to become disinfected [2].
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| ln Vivo |
In mice with active tumors, CNDAC (20 mg/kg; ip; daily for 10 days) demonstrated resistance [4].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Rad51D-deficient 51D1, Rad51D-complemented 51D1.3, wild-type AA8 and XRCC3-deficient irs1SF CHO cell Tested Concentrations: 0-1 μM Incubation Duration: 24 h Experimental Results: Inhibition of cell survival. The IC50 against Rad51D-deficient 51D1, Rad51D-complemented 51D1.3, wild-type AA8, and XRCC3-deficient irs1SF cell lines were 0.006, 0.32, 0.48, and 0.0053 μM, respectively. Cell proliferation assay [2] Cell Types: HL-60 and THP-1 Cell Tested Concentrations: 0-100 μM Incubation Duration: 3 days Experimental Results: Inhibitory effect on the proliferation of HL-60 and THP-1 cells, IC50 is 1.5832 μM and 0.84 μM, respectively. Apoptosis analysis[2] Cell Types: HL-60 and THP-1 Cell Tested Concentrations: 0, 0.5, 1, 2, 3, 4, 5 and 10 μM Incubation Duration: 3, 4, 5 and 6 days Experimental Results: Induction Apoptosis in both cells. Cell cycle analysis [3] Cell Types: HCT116 Tested Concentrations: 6 μM Incubation Duration: 48 hrs (hours) Experimental Results: 36% and 36% of cells were arrested in late S and G2/M phases respectively. |
| Animal Protocol |
Animal/Disease Models: CDF1 mouse, P388 tumor model [4]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection, daily for 10 days Experimental Results: Greatly improved survival time and survival rate. |
| References |
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| Additional Infomation |
Radgocitabine Hydrochloride is the hydrochloride salt form of radgocitabine, an analogue of the nucleoside deoxycytidine with potential antineoplastic activity. Upon administration, radgocitabine is incorporated into DNA and directly inhibits the activity of DNA polymerase, which may result in inhibition of DNA replication and cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis.
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| Molecular Formula |
C10H12N4O4.HCL
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|---|---|
| Molecular Weight |
288.68762
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| Exact Mass |
288.063
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| CAS # |
134665-72-8
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| Related CAS # |
CNDAC;135598-68-4
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| PubChem CID |
3035200
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| Appearance |
White to off-white solid powder
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| Boiling Point |
596.9ºC at 760mmHg
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| Flash Point |
314.8ºC
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| Vapour Pressure |
9.77E-17mmHg at 25°C
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
466
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)C#N.Cl
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| InChi Key |
PKGUOXDXRLGZBN-KUAPJGQRSA-N
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| InChi Code |
InChI=1S/C10H12N4O4.ClH/c11-3-5-8(16)6(4-15)18-9(5)14-2-1-7(12)13-10(14)17;/h1-2,5-6,8-9,15-16H,4H2,(H2,12,13,17);1H/t5-,6+,8-,9+;/m0./s1
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| Chemical Name |
(2R,3S,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)oxolane-3-carbonitrile;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~125 mg/mL (~432.99 mM)
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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 | 3.4639 mL | 17.3196 mL | 34.6392 mL | |
| 5 mM | 0.6928 mL | 3.4639 mL | 6.9278 mL | |
| 10 mM | 0.3464 mL | 1.7320 mL | 3.4639 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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