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Purity: ≥98%
FX-11 is a novel, potent and selective lactate dehydrogenase A (LDHA) inhibitor with anticancer activity. It inhibits LDHA with an IC50 of 23.3 μM in HeLa cells, and a Ki value of 8 μM. It inhibited tumor xenograft progression.
| ln Vitro |
Acetone-CoA pyruvylase, which is the substrate of FX-11 (9 μM) [2], is phosphorylated to demonstrate the activation of AMP. In P493 cells, FX-11 suppresses glycolysis and modifies cellular energy supplementing. In BxPc-3 and MIA PaCa-2 cells, FX-11 (0-100 μM, 72 h) limits cell growth [3].
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| ln Vivo |
FX-11 (42 μg/mouse; IP, once daily for 10–14 days) suppresses the formation of P493 tumors [2]. FX-11 (0–2 mg/kg, IP, once daily for three weeks) Standing
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| Cell Assay |
Western Blot Analysis [2]
Cell Types: P493 Cell Tested Concentrations: 9 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: ATP levels diminished, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase. Cell proliferation assay [3] Cell Types: BxPc-3 and MIA PaCa-2 Cell Tested Concentrations: 0-100 µM Incubation Duration: 72 hrs (hours) Experimental Results: diminished cell metabolic activity in a concentration-dependent manner, showing significant reduction in cell proliferation, BxPc- The IC50 values for 3 and MIA PaCa-2 cells were 49.27 µM and 60.54 µM, respectively. |
| Animal Protocol |
Animal/Disease Models: Male SCID (severe combined immunodeficient) mouse and RH-Foxn1nu (nude) mice (human P493 B cell xenografts) [2]
Doses: 42 μg /mouse (2.1 mg/kg) Route of Administration: IP; delays tumor growth [3]. one time/day for 10-14 days. Experimental Results: Significant inhibition of tumor growth and inhibition of tumor xenograft progression. Animal/Disease Models: Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group) [3] Doses: 2 mg/kg, 1 mg/kg+15 mg/kg TEPP- 46. 2 mg/kg+30 mg/kg TEPP-46 Route of Administration: intraperitoneal (ip) injection (100 µL), daily, for 3 weeks Experimental Results: LDHA activity in plasma and tumor lysates was Dramatically diminished; proliferation markers were Dramatically diminished The expression of Ki-67; a significant decrease in proliferation index was observed in tumor sections; and a significant delay in tumor growth. |
| References |
[1]. EC Calvaresi. Small molecule inhibitors of lactate dehydrogenase a as an anticancer strategy. 2014.
[2]. Le A, et, al. Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression. Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2037-42. [3]. Mohammad GH, et al. Targeting Pyruvate Kinase M2 and Lactate Dehydrogenase A Is an Effective Combination Strategy for the Treatment of Pancreatic Cancer. Cancers (Basel). 2019 Sep 16;11(9):1372. |
| Molecular Formula |
C22H22O4MO
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|---|---|
| Molecular Weight |
350.4077
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| CAS # |
213971-34-7
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| SMILES |
O=C(C1=C2C=C(CC3=CC=CC=C3)C(C)=CC2=C(CCC)C(O)=C1O)O
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| InChi Key |
LVPYVYFMCKYFCZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22O4/c1-3-7-16-17-10-13(2)15(11-14-8-5-4-6-9-14)12-18(17)19(22(25)26)21(24)20(16)23/h4-6,8-10,12,23-24H,3,7,11H2,1-2H3,(H,25,26)
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| Chemical Name |
7-Benzyl-2,3-dihydroxy-6-methyl-4-propylnaphthalene-1-carboxylic acid
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| Synonyms |
FX 11 FX11 FX-11
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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 : ~250 mg/mL (~713.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.94 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 (5.94 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 | 2.8538 mL | 14.2690 mL | 28.5380 mL | |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 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.
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