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100mg | ||
250mg | ||
500mg | ||
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Targets |
HSP90
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ln Vitro |
Conglobatin 6.25-100 μM; 48 h) significantly inhibits the proliferation of MCF-7 and SKBR3 cells with IC50s of 12.11 and 39.44 μM, respectively[2]. EC109, KYSE70, KYSE450, KYSE150, KYSE180, and KYSE510 cells exhibit inhibited cell proliferation in response to conglobatin, with IC50 values of 16.43, 15.89, 10.94, 10.50, 10.28, and 9.31 μM, respectively[3]. SKBR3 and MCF-7 cells exhibit a clear G2/M phase arrest when exposed to conglobatin (10–40 μM) for a 24-hour period. Conglobatin causes SKBR3 and MCF-7 cells to undergo apoptosis via caspase-dependent mechanisms[2]. Hsp90 client protein levels are decreased and proteasome-dependent degradation is induced by conglobatin (10–40 μM; 3–24 h)[2]. binds to Hsp90's N-terminal, inhibiting Hsp90/Cdc37 chaperone/co-chaperone interactions but having no effect on Hsp90's ability to bind ATP[2].
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ln Vivo |
In SKBR3 and MCF-7 human breast cancer xenograft models, conglobatin (50-200 mg/kg; ig q3d for 24 d) dose-dependently suppresses the growth of tumors[2]. In low-toxicity tumor xenograft models, EC109 and KYSE510, conglobatin (4–8 mg/kg; intraperitoneally every day for 21 days) suppresses the growth of tumors.[3]
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Cell Assay |
Cell Proliferation Assay[2]
Cell Types: SKBR3 and MCF-7 cells Tested Concentrations: 6.25, 12.5, 25, 50, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited the proliferation of SKBR3 and MCF-7 cells in a dose-dependent manner. Cell Cycle Analysis[2] Cell Types: SKBR3 and MCF-7 cells Tested Concentrations: 10, 20, 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Increased the G2/M cell population and diminished the population in the S and G0/G1 phases. Western Blot Analysis[2] Cell Types: SKBR3 and MCF-7 cells Tested Concentrations: 10, 20, 40 μM Incubation Duration: 3, 6, 12, 24 hrs (hours) Experimental Results: diminished the levels of the client proteins HER2, p-HER2, Raf-1, Akt, and p-Akt in a dose and time-dependent manner in SKBR3 cells. decreased the levels of the client proteins Raf-1, Akt, and p-Akt in a dose and time -dependent manner in MCF-7 cells. |
Animal Protocol |
Animal/Disease Models: BALB/c (nu/nu) athymic mice with SKBR3 and MCF-7 tumor xenograft[2]
Doses: 50, 100, 200 mg/kg Route of Administration: po (oral gavage) every 3 days for 24 days Experimental Results: demonstrated inhibition of tumor growth at a rate of 39.1%, 52.7%, and 67.5% in the SKBR3 cell line groups and 27.3%, 39.8%, 54.3% in the MCF-7 cell line groups at the three increasing doses, respectively. Was well tolerated. |
References |
[1]. Westley JW, et, al. Conglobatin, a novel macrolide dilactone from Streptomyces conglobatus ATCC 31005. J Antibiot (Tokyo). 1979 Sep;32(9):874-7.
[2]. Huang W, et, al. FW-04-806 inhibits proliferation and induces apoptosis in human breast cancer cells by binding to N-terminus of Hsp90 and disrupting Hsp90-Cdc37 complex formation. Mol Cancer. 2014 Jun 14;13:150. [3]. Li LY, et, al. Macrolide analog F806 suppresses esophageal squamous cell carcinoma (ESCC) by blocking β1 integrin activation. Oncotarget. 2015 Jun 30;6(18):15940-52. |
Molecular Formula |
C28H38N2O6
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Molecular Weight |
498.61
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CAS # |
72263-05-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C[C@H]1C=C(C)C(=O)O[C@@H](CC2=CN=CO2)[C@@H](C)C[C@@H](C)C=C(C)C(=O)O[C@@H](CC2=CN=CO2)[C@@H](C)C1 |c:2,12,31,t:10,21,29,&1:1,8,15,18,26,33|
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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 | 2.0056 mL | 10.0279 mL | 20.0558 mL | |
5 mM | 0.4011 mL | 2.0056 mL | 4.0112 mL | |
10 mM | 0.2006 mL | 1.0028 mL | 2.0056 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.