Size | Price | |
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500mg | ||
1g | ||
Other Sizes |
ln Vitro |
Under stress, apogossypolone (ApoG2) exhibits enhanced stability [1]. In a dose-dependent manner, apogossypolone (0-1 µM) suppresses the proliferation of WSU-DLCL2 cells after 72 or 96 hours [1]. Apogossypolone (0-5 µM, 24 or 48 hours) causes caspase-3, caspase-9, and PARP cleavage and prevents anti- and pro-apoptotic Bcl-2 family members from forming heterodimers [1]. In WSU-DLCL2 cells, apogossypolone (0-8 µM, 0-72 hours) causes apoptosis in a dose- and time-dependent manner [1]. In HCC cells, apogossypolone (0–10 µM, 0–24 hours) stimulates the production of ROS and induces autophagy [2].
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ln Vivo |
Apogossypolone (ApoG2) (120 mg/kg; intravenously or orally; once daily for 5 days) efficiently reduces the proliferation of diffuse large cell lymphoma cells without harm [1].
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Cell Assay |
Cell proliferation assay[1]
Cell Types: WSU-DLCL2 Tested Concentrations: 250, 350, 500 and 1000 nM Incubation Duration: 96 hrs (hours) for cell counting, 72 hrs (hours) for MTT Experimental Results: Inhibition of growth in a dose-dependent manner. The 50% growth inhibitory concentration (IC50) is approximately 350 nM. Western Blot Analysis[1] Cell Types: WSU-DLCL2 Tested Concentrations: 0.35, 0.5, 1 and 5 µM Incubation Duration: 24 or 48 hrs (hours) Experimental Results: Blocks heterodimerization between Bcl-XL and Bim in a concentration-dependent manner form. Resulting in activation of caspase-3, caspase-9 and PARP cleavage. Apoptosis analysis[1] Cell Types: WSU-DLCL2 Tested Concentrations: 0, 1, 2, 4 and 8 µM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Apoptosis was induced in a time- and dose-dependent manner. Autophagy assay[2] Cell Types: HepG2 and Hep3B Tested Concentrations: 1.25, 2.5, 5 and 10 µM Incubation Duration: 6, 12, 18 and 24 hrs (hours) Experimental Results: Induction of LC3 (Light Chain 3)- II A way to transform time dependence. |
Animal Protocol |
Animal/Disease Models: Fourweeks old female ICR-SCID (severe combined immunodeficient) mouse received 107 WSU-DLCL2 cells (serum-free RPMI 1640) per mouse subcutaneously (sc) (sc) (sc) in each flank region [1]
Doses: 120 mg/kg administered Method: intravenous (iv) (iv)injection or daily administration for five days. Experimental Results: Inhibited the growth of WSU-DLCL2 and Dramatically diminished tumor weight. Animal/Disease Models: non-tumor SCID (severe combined immunodeficient) mouse [1] Doses: 160 mg/kg Route of Administration: intravenous (iv) (iv)injection or daily administration for five days Experimental Results: Up to 800 mg/kg was well tolerated by mice. demonstrated no obvious signs of toxicity. |
References |
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Molecular Formula |
C28H26O8
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Molecular Weight |
490.50124
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Exact Mass |
490.163
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CAS # |
886578-07-0
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PubChem CID |
135513044
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Appearance |
Typically exists as solid at room temperature
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LogP |
4.847
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Hydrogen Bond Donor Count |
4
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Hydrogen Bond Acceptor Count |
8
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Rotatable Bond Count |
3
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Heavy Atom Count |
36
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Complexity |
1120
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Defined Atom Stereocenter Count |
0
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SMILES |
O=C1C(C(C2=O)=C(C)C(C3=C2C=C(O)C(O)=C3C(C)C)=O)=C(C)C(C4=C1C=C(O)C(O)=C4C(C)C)=O
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InChi Key |
PXSGRWNXASCGTJ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H26O8/c1-9(2)17-21-13(7-15(29)27(17)35)25(33)19(11(5)23(21)31)20-12(6)24(32)22-14(26(20)34)8-16(30)28(36)18(22)10(3)4/h7-10,29,31,33,35H,1-6H3
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Chemical Name |
3-methyl-5-propan-2-yl-2-(1,4,6,7-tetrahydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)naphthalene-1,4,6,7-tetrone
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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 | 2.0387 mL | 10.1937 mL | 20.3874 mL | |
5 mM | 0.4077 mL | 2.0387 mL | 4.0775 mL | |
10 mM | 0.2039 mL | 1.0194 mL | 2.0387 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.