| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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| ln Vitro |
BX-320 attaches itself to PDK1's ATP binding site. Additionally, BX-320 inhibits CDK2b/cyclin E, Chck1, c-Kit, KDR, PKA, GSK3β, and PKC with IC50 values of 0.82, 0.89, 1.4, 1.5, 4.0, and 5.7 μM, in that order[1]. In addition to inhibiting the anchorage-dependent development of several tumor cell lines in culture or inducing apoptosis, BX-320 disrupts PDK1/Akt signaling in tumor cells[1]. BX-320 causes apoptosis and suppresses the development of MDA-468 breast cancer cells (IC50=0.6 μM). After 48 hours of treatment, BX-320 causes a 12-fold increase of caspase-3/7 activity (IC50=0.5 μm), suggesting a potent proapoptotic response[1]. For 18 hours, BX-320 (0.3–10 μM) significantly lowers the levels of p-Thr308-Akt and p-Thr386-S6K1[1].
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| ln Vivo |
Blood-borne metastases model: BX-320 (oral dose of 200 mg/kg, twice day for 21 days) is effective. Following the injection of tumor cells into the tail vein, BX-320 suppresses the formation of LOX melanoma tumors in the lungs of naked mice. BX-320 is effective in an in vivo tumor model, which may indicate that it inhibits the growth of the tumor once it has been implanted in the lung or the productive implantation of tumor cells[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MDA-468 breast cancer cells Tested Concentrations: 31.6 nM, 100 nM, 316.22 nM, 1 μM, 3.162 μM, 10 μM, and 31.6 μM Incubation Duration: 72 hrs (hours) Experimental Results: Blocked the growth of MDA-468 cells (IC50=0.6 μM), which are PTEN -negative breast tumor cells expressing high levels of activated Akt. Western Blot Analysis[1] Cell Types: PC-3 cells Tested Concentrations: 0, 0.3, 1, 3, 10 μM Incubation Duration: 18 hrs (hours) Experimental Results: diminished the amount of both phospho -Thr308-Akt and phospho-Thr386-S6K1. |
| Animal Protocol |
Animal/Disease Models: Athymic (nu/nu ) female mice, 6-8 weeks old[1]
Doses: 200 mg/kg; dose volume was 10 mL/kg Route of Administration: po (oral gavage) twice (two times) daily (12 h apart) Experimental Results: Dramatically inhibited the growth of lung tumors in this model. |
| References |
[1]. Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.
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| Molecular Formula |
C23H31BRN8O3
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|---|---|
| Molecular Weight |
547.45
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| CAS # |
702676-93-5
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| SMILES |
CC(C(N)=O)(C(NCCCN=C1C(Br)=CN=C(N1)NC2=CC(NC(N3CCCC3)=O)=CC=C2)=O)C
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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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8267 mL | 9.1333 mL | 18.2665 mL | |
| 5 mM | 0.3653 mL | 1.8267 mL | 3.6533 mL | |
| 10 mM | 0.1827 mL | 0.9133 mL | 1.8267 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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