Size | Price | |
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100mg | ||
250mg | ||
500mg |
Targets |
LeuRS and RagD interaction ( IC50 = 46.11 nM ); LeuRS and RagD interaction ( Kd = 42.1 nM )
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ln Vitro |
BC-LI-0186 inhibits both mTORC1 activity and the lysosomal localization of LRS by binding to the RagD interacting site of LRS. Additionally, BC-LI-0186 successfully inhibits the growth of rapamycin-resistant cancer cells as well as the activity of MTOR mutants linked to cancer.[1]
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ln Vivo |
BC-LI-0186 (intraperitoneal injection; 50 mg/kg; for two weeks; administered alone or in combination with cisplatin alone; administered five days a week) shows antitumor effects and, in an animal model of lung cancer with LSL K-ras G12D, significantly reduces tumor size when compared with treatment with vehicle.[1]
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Cell Assay |
Leucine-free medium is used to starve the cells for ninety minutes. After that, they are placed in serum-free media for fifteen minutes, one and a half hours, or six hours. Additionally, the matching antibodies are used to analyze the cell lysates.
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Animal Protocol |
K-ras mouse lung cancer model, LSL K-ras G12D lung cancer mouse model
50 mg/kg i.p. |
References |
Molecular Formula |
C22H27N3O4S
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Molecular Weight |
429.53
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Exact Mass |
429.17
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Elemental Analysis |
C, 61.52; H, 6.34; N, 9.78; O, 14.90; S, 7.46
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CAS # |
695207-56-8
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Appearance |
Solid powder
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SMILES |
CC1=C(C(=O)N(N1C)C2=CC=C(C=C2)S(=O)(=O)NCCOC3=CC=CC=C3)C(C)C
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InChi Key |
SQYWMHPZMHDCHP-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H27N3O4S/c1-16(2)21-17(3)24(4)25(22(21)26)18-10-12-20(13-11-18)30(27,28)23-14-15-29-19-8-6-5-7-9-19/h5-13,16,23H,14-15H2,1-4H3
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Chemical Name |
4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
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Synonyms |
BC-LI 0186; BC-LI-0186; BC-LI0186; BCLI 0186; BCLI0186; BCLI-0186
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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) |
DMSO : 86~125 mg/mL (200.2~291.0 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3281 mL | 11.6406 mL | 23.2813 mL | |
5 mM | 0.4656 mL | 2.3281 mL | 4.6563 mL | |
10 mM | 0.2328 mL | 1.1641 mL | 2.3281 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.
Determination of BC-LI-0186 docking site. a Structural modeling of human cytoplasmic LRS. Nat Commun . 2017 Sep 29;8(1):732. td> |
Effect of BC-LI-0186 on cancer cell death. a SW620 cells were treated with DMSO (Con), rapamycin (100 nM), BC-LI-0186 (10 μM), or 5-FU (10 μM) for 24 h. Nat Commun . 2017 Sep 29;8(1):732. td> |