JQ-1 carboxylic acid, a type of (+)-JQ-1 derivative, is a potent BET bromodomain inhibitor for downregulating PD-L1 expression on the surface of tumor cells. JQ-1 carboxylic acid can be used as a precursor to synthesize PROTACs, which targets BET bromodomains.
Cell Experiment | |
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Cell lines | MC 11060 cells |
Preparation method | Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism). |
Concentrations | ~500 nM |
Incubation time | 48 hours |
Animal Experiment | |
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Animal models | Mice bearing NMC 797 xenografts |
Formulation | 5% DMSO in 5% dextrose |
Dosages | 50 mg/kg |
Administration | intraperitoneal injection |
Molecular Weight | 400.88 |
Formula | C19H17ClN4O2S |
CAS Number | 202592-23-2 |
Solubility (25°C) | DMSO 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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