Size | Price | |
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100mg | ||
250mg | ||
500mg |
ln Vitro |
The growth of cancer cells is inhibited by BS-181 diHClide (0–40 μM; 72 hours), which also inhibits the growth of breast cancer cell lines (IC50 values: 15.1 μM–20 μM) and colorectal cancer cell lines (IC50 values: 11.5 μM–20 μM). 15.3 μM, with IC50 values against cell lines of lung cancer, osteosarcoma, prostate cancer, and liver cancer, respectively, ranging from 11.5 μM to 37.3 μM [1]. Phosphorylation of RNA polymerase II's C-terminal domain (CTD) serine 5 (P-Ser5) is inhibited by BS-181 dihydrochloride (0-50 μM; 4 hours). While it has no effect on other CDKs or cyclins, it downregulates the expression of CDK4 and cyclin D1 [1]. At low concentrations, the number of cells in the G1 phase increased and the number in the S and G2/M phases decreased when exposed to BS-181 dihydrochloride (0-50 μM; 24 hours). Higher concentrations, however, cause cells to accumulate in the sub-G1 phase, which is indicative of apoptosis [1].
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ln Vivo |
Mice treated with BS-181 dihydrochloride (10 mg/kg, 20 mg/kg; single dose) responded well to the medication and their body weight did not significantly change [1]. Tumor growth is dosage-dependently inhibited by BS-181 dihydrochloride (ip; 5 mg/kg or 10 mg/kg twice daily; total daily dose 10 mg/kg or 20 mg/kg; 14 days). Ten mg/kg and twenty mg/kg/day, respectively, slowed tumor growth by 25% and 50% as compared to the control group [1].
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Cell Assay |
Cell proliferation experiment [1]
Cell Types: Breast cancer Cell Types: MCF-7, MDA-MB-231, T47D, ZR-75-1, etc. Colorectal cancer Cell Types: COLO-205, HCT-116, HCT-116 ( p53-/-) Lung cancer Cell Types: A549, NCI-460 Osteosarcoma Cell Types: U2OS, SaOS2 Prostate cancer Cell Types: PC3, LNCaP Tested Concentrations: 0-40 μM Incubation Duration: 72 hrs (hours) Experimental Results: A group of cells with anti-proliferative activity systems, including breast, lung, prostate and colorectal cancer. Western Blot Analysis[1] Cell Types: Breast Cancer Cell Types: MCF-7 Cell Tested Concentrations: 0 μM; 25 μM; 50 μM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibition of phosphorylation of CDK7 substrate. Apoptosis analysis [1] Cell Types: Breast cancer Cell Types: MCF-7 Cell Tested Concentrations: 0 μM; 25 μM; 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Causes cell G1 phase arrest and apoptosis. |
Animal Protocol |
Animal/Disease Models: 7weeks old female nu/nu-BALB/c athymic nude mice, MCF-7 cells [1]
Doses: 5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a day or one time/day in total; 14-day Experimental Results: Dramatically inhibited tumor growth. |
References |
[1]. Ali S et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009 Aug 1;69(15):6208-15.
[2]. Wang BY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016 Mar 16;10:1181-9. |
Molecular Formula |
C22H34CL2N6
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Molecular Weight |
453.4516
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CAS # |
1883548-83-1
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Related CAS # |
BS-181 hydrochloride;1397219-81-6;BS-181;1092443-52-1
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SMILES |
Cl[H].Cl[H].N12C(=C([H])C(=NC1=C(C([H])=N2)C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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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 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 | 2.2053 mL | 11.0266 mL | 22.0531 mL | |
5 mM | 0.4411 mL | 2.2053 mL | 4.4106 mL | |
10 mM | 0.2205 mL | 1.1027 mL | 2.2053 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.