| Size | Price | Stock | Qty |
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| 5mg |
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| ln Vitro |
WBC100 specifically destroys c-Myc overexpressing cancer cells Mia-paca2, H9, and MOLM-13, as well as low-expressing c-Myc normal human cell lines L02, MRC-5, and WI38. The values of IC50 against cancer cells that overexpress are 61×10-9, 17×10-9, and 16×10-9 M, in that order. For normal cell lines, the IC50 values are, in order, 2205 × 10-9, 151 × 10-9, and 570 × 10-9 M [1]. WBC100 (0-320 nM; 24 hours) dose-dependently decreased the amounts of c-Myc protein in MOLM-13 and Mia-paca2 cells, but had no discernible effect on XPB, Rpb1, or STAT3. Furthermore, WBC100-induced c-Myc protein can be saved by MG132 [1].
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| ln Vivo |
WBC100 (po; 0.1–0.4 mg/kg; twice daily; 21 days) demonstrates anticancer efficacy that is dose-dependent. In vivo WBC100 treatment of high or medium doses (0.4/0.2 mg/kg) completely eliminated MOLM-13-luciferase cells, and by day 35, all animals were disease-free. Furthermore, WBC100 has been shown to considerably reduce tumor growth and increase survival in leukemia mice at modest dosages (0.1 mg/kg) [1]. Refractory MOLM-13-luciferase cells are eliminated in vivo by WBC100 (po; 0.4-0.8 mg/kg; once daily for 14 days); nevertheless, +)-JQ1 (50 mg/kg, i.p., daily Once, for 14 days) is ineffective in preventing tumor growth. Compared to the c-Myc transcription inhibitor (+)-JQ1, WBC100 has greater anti-tumor efficacy [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: c-Myc overexpressing cancer cells: Mia-paca2, H9, and MOLM-13 cell c- Myc-low normal human Cell Types: L02, MRC-5 and WI38 Tested Concentrations: Incubation Duration: 72 hrs (hours) Experimental Results: Preferentially killed c-Myc overexpressing cancer cells. Western Blot Analysis[1] Cell Types: Mia-paca2 cells, MOLM-13 cell Tested Concentrations: 0 nM, 20 nM, 40 nM, 80 nM, 160 nM, 320 nM Incubation Duration: 24 hrs (hours) Experimental Results: Selectively induced degradation of c-Myc protein through E3 ubiquitin ligase CHIP mediated 26S proteasome pathway. |
| Animal Protocol |
Animal/Disease Models: Orthotopic human AML model using NOD/SCID/IL2Rγ-/- (NSG) mice with refractory MOLM-13-luciferase cells with high c-Myc levels
Doses: 0.1 mg/kg; 0.2 mg/kg; 0.4 mg/kg Route of Administration: po; 0.1-0.4 mg/kg; twice (two times) daily; 21 days Experimental Results: Regresses c-Myc overexpressing refractory acute myeloid leukemia model. |
| References |
| Molecular Formula |
C25H33NO7
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|---|---|
| Molecular Weight |
459.532027959824
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| Exact Mass |
459.225
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| CAS # |
2095780-08-6
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| PubChem CID |
134236278
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| Appearance |
White to off-white solid powder
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(C)[C@H](C(=O)O[C@H]1[C@@]23[C@@H](O2)C[C@H]4C5=C(CC[C@@]4([C@]36[C@@H](O6)[C@H]7[C@@]1(O7)C(C)C)C)C(=O)OC5)N
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| InChi Key |
OWLJDBBFRJXPGM-VBIGTWTASA-N
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| InChi Code |
InChI=1S/C25H33NO7/c1-10(2)16(26)20(28)30-21-23(11(3)4)17(32-23)18-25(33-18)22(5)7-6-12-13(9-29-19(12)27)14(22)8-15-24(21,25)31-15/h10-11,14-18,21H,6-9,26H2,1-5H3/t14-,15-,16+,17-,18-,21+,22-,23-,24+,25+/m0/s1
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| Chemical Name |
[(1S,2S,4S,5S,7S,8R,9R,11S,13S)-1-methyl-17-oxo-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-8-yl] (2R)-2-amino-3-methylbutanoate
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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 | 2.1761 mL | 10.8807 mL | 21.7614 mL | |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3523 mL | |
| 10 mM | 0.2176 mL | 1.0881 mL | 2.1761 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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