7ACC2CAS# 1472624-85-3 |
- PI 828
Catalog No.:BCC7494
CAS No.:942289-87-4
Quality Control & MSDS
3D structure
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| Cas No. | 1472624-85-3 | SDF | Download SDF |
| PubChem ID | 72696735 | Appearance | Powder |
| Formula | C18H15NO4 | M.Wt | 309.32 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (161.64 mM; Need ultrasonic) | ||
| Chemical Name | 7-[benzyl(methyl)amino]-2-oxochromene-3-carboxylic acid | ||
| SMILES | CN(CC1=CC=CC=C1)C2=CC3=C(C=C2)C=C(C(=O)O3)C(=O)O | ||
| Standard InChIKey | XTKDQPFUOFAMRL-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H15NO4/c1-19(11-12-5-3-2-4-6-12)14-8-7-13-9-15(17(20)21)18(22)23-16(13)10-14/h2-10H,11H2,1H3,(H,20,21) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
7ACC2 Dilution Calculator
7ACC2 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2329 mL | 16.1645 mL | 32.329 mL | 64.658 mL | 80.8224 mL |
| 5 mM | 0.6466 mL | 3.2329 mL | 6.4658 mL | 12.9316 mL | 16.1645 mL |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2329 mL | 6.4658 mL | 8.0822 mL |
| 50 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.2932 mL | 1.6164 mL |
| 100 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.6466 mL | 0.8082 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells. IC50 value: 11 nM ([14C]-lactate influx) [1] Target: MCT inhibitor; lactate transport inhibitor 7ACC2 did not influence the prothrombin time which, together with a good in vitro ADME profile, supports the potential of this new family of compounds to act as anticancer drugs through inhibition of lactate flux.
References:
[1]. Draoui N, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorg Med Chem. 2013 Nov 15;21(22):7107-17.
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Killing two birds with one stone: Blocking the mitochondrial pyruvate carrier to inhibit lactate uptake by cancer cells and radiosensitize tumors.[Pubmed:30250917]
Mol Cell Oncol. 2018 May 22;5(4):e1465016.
Lactate-based metabolic symbiosis between glycolytic and oxidative cancer cells is known to facilitate tumor growth. We have recently demonstrated that 7ACC2 blocks extracellular lactate uptake via the inhibition of mitochondrial pyruvate carrier. 7ACC2 also prevents compensatory glucose oxidation, induces tumor reoxygenation and potentiates radiotherapy, making it a promising anticancer drug.
Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects.[Pubmed:29572438]
Nat Commun. 2018 Mar 23;9(1):1208.
Lactate exchange between glycolytic and oxidative cancer cells is proposed to optimize tumor growth. Blocking lactate uptake through monocarboxylate transporter 1 (MCT1) represents an attractive therapeutic strategy but may stimulate glucose consumption by oxidative cancer cells. We report here that inhibition of mitochondrial pyruvate carrier (MPC) activity fulfils the tasks of blocking lactate use while preventing glucose oxidative metabolism. Using in vitro (13)C-glucose and in vivo hyperpolarized (13)C-pyruvate, we identify 7ACC2 as a potent inhibitor of mitochondrial pyruvate transport which consecutively blocks extracellular lactate uptake by promoting intracellular pyruvate accumulation. Also, while in spheroids MCT1 inhibition leads to cytostatic effects, MPC activity inhibition induces cytotoxic effects together with glycolysis stimulation and uncompensated inhibition of mitochondrial respiration. Hypoxia reduction obtained with 7ACC2 is further shown to sensitize tumor xenografts to radiotherapy. This study positions MPC as a control point for lactate metabolism and expands on the anticancer potential of MPC inhibition.
