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| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
PROTAC B-Raf degrader 1 (compound 2) had IC50 values of 2.7 μM, 21.21 μM, 18.70 μM, 41.11 μM, and 22.68 μM against MCF-7, MDA-MB-231, HepG2, LO2, and B16 cells, respectively [1]. By enlisting the ubiquitin-proteasome system, PROTAC B-Raf degrader 1 (5 or 10 μM) can hasten B-Raf degradation and consequently impact the expression of B-Raf downstream protein Mcl-1 [1]. Following a 24-hour incubation period with a 20 μM concentration of PROTAC B-Raf degrader 1, the MCF-7 cells exhibited an apoptotic rate of 76.70% (early apoptosis 64.00%, late apoptosis 12.70%) [1]. The cell cycle is stopped in the G2/M phase by PROTAC B-Raf degrader 1 [1].
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells. Tested Concentrations: 0-200 μM. Incubation Duration: 72 hrs (hours). Experimental Results: The IC50 values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively. Western Blot Analysis[1] Cell Types: Human MCF-7 breast cancer cell line. Tested Concentrations: 5 or 10 μM. Incubation Duration: 24 hrs (hours). Experimental Results: Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1. Apoptosis Analysis[1] Cell Types: Human MCF-7 breast cancer cell line. Tested Concentrations: 2.7-20 μM. Incubation Duration: 24 hrs (hours). Experimental Results: Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM. Cell Cycle Analysis[1] Cell Types: Human MCF-7 breast cancer cell line. Tested Concentrations: 20 μM. Incubation Duration: 24 hrs (hours). Experimental Results: 1.94% cells were |
| References |
[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Mar 19;87:191-199.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.27 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 25.0 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: ≥ 2.5 mg/mL (3.27 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 25.0 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.) |
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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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