| ln Vitro |
NV914 (3–48 μM; 24 h) did not induce NTC readthrough in HCT116 cells because no high molecular weight p53 band was detected after treatment with doxorubicin [1]. NV914 (3–48 μM; 24 h) did not alter the nuclear localization of p53 in HCT116 cells after treatment with doxorubicin [1]. NV914 (3–48 μM; 24 h) did not impair p53 function in HCT116 cells after treatment with doxorubicin (measured by p21 mRNA expression) [1]. NV914 (12–100 μM; 24 or 72 h) did not induce NTC readthrough in 16HBE cells because no high molecular weight Cys-C or β2M band was detected after treatment [1]. NV914 (6-24 μM; 24 h) can induce premature readthrough of UGA stop codons in HeLa cells transfected with pFLuc190UGA, while FTSJ1 overexpression can antagonize this effect [3]. NV914 (12 μM; 24 h) can induce premature readthrough of W1282X UGA stop codons in IB3.1 cystic fibrosis cells, while FTSJ1 overexpression can reduce this effect [3].
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| ln Vivo |
NV914 (2000 mg/kg; orally; single dose) was well tolerated in healthy C57BL/6 mice with only transient toxic symptoms and no obvious organ damage, and was therefore classified as GHS Category 5 (low health risk)[2].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: HCT116 colon cancer cells Tested Concentrations: 3-48 μM Incubation Duration: 24 hours Experimental Results: Compared with samples treated with doxorubicin alone, the p53 protein level was slightly decreased in cells treated with NV914 and doxorubicin; no p53 band with a high molecular weight was shown (indicating natural stop codon [NTC] readout). Immunofluorescence [1] Cell Types: HCT116 colon cancer cells Tested Concentrations: 3-48 μM Incubation Duration: 24 hours Experimental Results: In all cell samples treated with doxorubicin and NV914, the p53 fluorescence signal was localized in the cell nucleus; no significant changes in p53 nuclear localization were observed. Western Blot Analysis [1] Cell Types: 16HBE human bronchial epithelial cells Tested Concentrations: 12-100 μM (treated for 24 hours); 12-100 μM (treated for 72 hours, replaced every 24 hours) Incubation Duration: 24 hours; 72 hours (replaced every 24 hours) Experimental Results: No bands corresponding to the high molecular weight forms of Cys-C or β2M were detected in cells treated with NV914 for 24 or 72 hours. |
| Animal Protocol |
Animal/Disease Models:C57BL/6 (both male and female, 6-8 weeks old, weight 18±4 g) [2]
Doses: 2000 mg/kg Route of Administration: Oral; single dose Experimental Results: No deaths were observed within 14 days. Of the 6 treated mice, 5 showed decreased activity, 4 showed hyperactivity and abdominal pain, 3 showed tremors and convulsions, and 2 showed itching and scratching; all toxic symptoms subsided within 3 hours after treatment. No significant difference in weight gain pattern was detected compared with the control group. No significant morphological changes were found in the analyzed organs except for slightly abnormal neutrophil maturation and mild erythroid proliferation in two bone marrow samples. |
| References |
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| CAS # |
2341941-41-9
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|---|---|
| Appearance |
White to off-white solid
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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) |
DMSO : ~100 mg/mL (~224.63 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
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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