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 | |
|---|---|
| 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 | |
|---|---|
| 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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