Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg |
ln Vitro |
Naphthylfluorescein (compound 19) inhibits HIF-1 reporter gene activity in a concentration-dependent manner (0-10 μM; 24 hours) [1].
|
---|---|
ln Vivo |
Naphthafluorescein (Compound 19) (100 mg/kg; i.p.; once daily for 5 days followed by 2 days off for 2 weeks) does not induce weight loss or major histological abnormalities in the lungs, liver, and kidneys, or Causes severe symptoms and harmful consequences in mice for at least two weeks [1]. Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 days, followed by 2 days of rest for 2 weeks) greatly decreased tumor growth of subcutaneously injected E0771 cells and considerably diminished MDA- Tumor growth of MB-231 and MDA-MB-231. AsPC-1 cells in immunodeficient mice. In turn, naphthylfluorescein did not decrease tumor growth in FIH-1-depleted MDA-MB-231 cells [1]. Naphthafluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 days followed by 2 days rest for 2 weeks) suppresses tumor development in human cancer cells in a FIH-1-dependent way [1] .
|
Cell Assay |
Cell viability assay [1]
Cell Types: HT1080 Cell Tested Concentrations: 0-10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically inhibited HIF-1 reporter gene activity in a concentration-dependent manner. |
Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice (8 weeks) [1]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 5 days, then rest for 2 days for 2 weeks. Experimental Results: Mice were There was no weight loss or obvious histological abnormalities in the lungs, liver, or kidneys, or serious adverse reactions for at least 2 weeks. Animal/Disease Models: Female C57BL/6J mice (E0771) and BALB/c nude mice (HT1080, MDA-MB-231 and AsPC-1) (6 weeks) [1] Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection ; one time/day for 5 days, then 2 days off for 2 weeks. Experimental Results: Dramatically inhibited tumor growth of subcutaneously (sc) (sc) injected E0771 cells and Dramatically attenuated the growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. Tumor growth. In turn, naphthylfluorescein did not attenuate tumor growth in FIH-1-depleted MDA-MB-231 cells. |
References |
[1]. Sakamoto T, et al. Pharmacological inhibition of Mint3 attenuates tumour growth, metastasis, and endotoxic shock. Commun Biol. 2021;4(1):1165. Published 2021 Oct 7.
[2]. Arroyo AD, et al. Development of fluorinated naphthofluoresceins for Cerenkov imaging. J Fluor Chem. 2019;225:27-34. |
Molecular Formula |
C28H16O5
|
---|---|
Molecular Weight |
432.424
|
CAS # |
61419-02-1
|
SMILES |
C1=CC=C2C(=C1)C(=O)OC23C4=C(C5=CC=C(C=C5C=C4)O)OC6=C3C=CC7=CC(=CC=C76)O
|
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)
|
Solubility (In Vitro) |
DMSO : ~125 mg/mL (~289.07 mM)
|
---|---|
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 | 2.3126 mL | 11.5628 mL | 23.1257 mL | |
5 mM | 0.4625 mL | 2.3126 mL | 4.6251 mL | |
10 mM | 0.2313 mL | 1.1563 mL | 2.3126 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.