| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| ln Vitro |
NCI-006 (0-1 μM) inhibited the activity of human lactate dehydrogenase (hLDH) and lactate dehydrogenase isoenzymes 2, 3, 4, 5 in HEK293T cells and mouse isoenzymes 1, 2, 3, 4, 5, but did not inhibit the activity of malate dehydrogenase (MDH) and succinate dehydrogenase (SDH) isolated from human kidney [3]. NCI-006 (0.2-5 μM, 2 h) reduced the NAD/NADH ratio in MIA PaCa-2 and HT29 cells and affected lactate secretion in mouse (m) and human (h) erythrocytes (RBCs) and MIA PaCa-2 and HT29 cells, with EC50 values of 1.6, 2.1, 0.37, and 0.53 μM, respectively [3]. NCI-006 (0-10 μM, 0-180 min) reduced the basal extracellular acidification rate (ECAR) in a time-dependent manner at the lowest concentration of 1 μM, and inhibited glycolysis at concentrations ≥ 1 μM, while increasing the basal oxygen consumption rate (OCR) in MIA PaCa-2 cells [3]. NCI-006 (1 μM) in combination with IACS-010759 reduced the cell viability of MIA PaCa-2, HCT116 and MKN45 cells [3][6]. NCI-006 (5 μM) reduced the OCR, ECAR and glycoATP production rate in HCT116 and MKN45 cells, but did not affect the mitochondrial ATP production rate or the total ATP production rate, nor did it increase the ATP production rate during mitosis, but its combination with IACS-010759 significantly increased the glycoATP production rate [6]. NCI-006 (72 hours) inhibited the proliferation of Ewing sarcoma cell lines with an IC50 ranging from 100 nmol/L (TC71 and TC32) to 1 μmol/L (RDES and EW8), but had no effect on rhabdomyosarcoma and osteosarcoma with an IC50 of 1,037 nmol/L [7]. NCI-006 dose-dependently inhibited LDH activity in TC71, TC32, and EW8 cells with an IC50 of approximately 100 nmol/L [7]. NCI-006 (0.1–10 μM, 2 hours) inhibited ECAR in TC71 and EW8 cells [7].
|
|---|---|
| ln Vivo |
NCI-006 (0-200 mg/kg, neck/intravenous injection, once) reduced LDH activity in female athymic nude mice within 2 hours [3]. NCI-006 (50 mg/kg, neck/intravenous injection, once; intravenous injection, every other day, for 1 or 2 weeks) blocked tumor LDH activity in MIA PaCa-2/HT29 female athymic nude mice, resulting in a decrease in the conversion rate of pyruvate to pyruvate, an increase in the permeation of pyruvate to bicarbonate and mitochondrial oxidation, while no significant increase in transaminase-mediated pyruvate to pyruvate conversion was observed, thereby terminating tumor growth [3]. NCI-006 (40 mg/kg, intravenously, 2/3 times a week for 1/2 weeks) alone did not inhibit tumor growth, but when used with IACS-010759, it inhibited HCT116 and combined with MKN45 NCI-006 (50 mg/kg, once or twice daily for 3 weeks) had little effect on tumor growth in TC71, TC32 and EW8 xenografted female Fox Chase SCID beige mice[7].
|
| Animal Protocol |
Animal/Disease Models: Female athymic nude mice (20-25 g)[3]
Doses: 0 mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg Route of Administration: p.o., once Experimental Results: Dose-dependent reduced LDH activity at 2 h, but in most cases, recovery to baseline levels by 24 h, 75%-80% of baseline at 24 h, with maximal inhibition maintained at 8 h. Animal/Disease Models: Female athymic nude mice (20-25 g)[3] Doses: 0 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg Route of Administration: i.v., once Experimental Results: Dose-dependent reduced LDH activity at 2 h, but in most cases, recovery to baseline levels by 24 h. Animal/Disease Models: MIA PaCa-2 tumor female athymic nude mice (20-25 g)[3] Doses: 50 mg/kg Route of Administration: p.o./i.v., once; i.v., every other day for 1 week (three injections, Monday, Wednesday, and Friday), or for 2 weeks (six injections) with a break of 1 week between cycles. Experimental Results: Inhibited LDH by 80% at intratumoral drug levels of approximately 20 μM. Dose dependently suppressed the tumor [13C]lactate/[13C]pyruvate ratio, did not affect the [13C]lactate/[13C]pyruvate ratio in MIA PaCa-2 tumors (up to 7 h after drug administration). Slowed the growth of MIA PaCa-2 xenografts without a marked effect on mouse body weight. Reduced conversion of [13C]pyruvate to both [13C]lactate and [13C]bicarbonate, more significantly inhibits tumor growth in combination with IACS-010759. Animal/Disease Models: HT29 tumor female athymic nude mice (20-25 g)[3] Doses: 50 mg/kg Route of Administration: i.v., once Experimental Results: Decreased the [13C]Lac/[13C]Pyr ratio by 74.7%. More significantly inhibits tumor growth when combined with Metformin. Animal/Disease Models: HCT116 (5×106) xenografts nude mice (18-24 g, six-week-old female KSN/slc athymic)[6] Doses: 40 mg/kg Route of Administration: i.v., 3 times a week, 1 weeks Experimental Results: Treatment alone did not inhibit tumor growth, inhibited tumor growth and transiently and significantly increased AST, ALT, amylase, lipase, creatinine, and bilirubin levels in combination with IACS-010759. Decreased the 13C-L/P ratio, increased ROS levels. Animal/Disease Models: MKN45 xenografts nude mice (18-24 g, six-week-old female KSN/slc athymic)[6] Doses: 40 mg/kg Route of Administration: i.v., 2 times a week, 2 weeks Experimental Results: Treatment alone did not inhibit tumor growth, inhibited tumor growth and transiently and significantly increased AST, ALT, amylase, lipase, creatinine, and bilirubin levels in combination with IACS-010759. Decreased the 13C-L/P ratio. Animal/Disease Models: TC71, TC32, and EW8 xenografts female Fox Chase SCID beige mice [7] Doses: 50 mg/kg Route of Administration: p.o., once or twice daily, 3 weeks Experimental Results: Had little change in tumor growth. |
| References |
| Molecular Formula |
C31H24F2N4O4S3
|
|---|---|
| Molecular Weight |
650.74
|
| CAS # |
1964516-64-0
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~76.84 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5367 mL | 7.6836 mL | 15.3671 mL | |
| 5 mM | 0.3073 mL | 1.5367 mL | 3.0734 mL | |
| 10 mM | 0.1537 mL | 0.7684 mL | 1.5367 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
