| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
ASCT2[1]
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|---|---|
| ln Vitro |
V-9302 hydrochloride is 100 times more effective than γ-L-glutamyl-p-nitroanilide and inhibits ASCT2-mediated glutamine absorption in human cells in a concentration-dependent manner [1]. enhanced oxidative stress, reduced cancer cell growth and proliferation, and enhanced cell death are the outcomes of pharmacologically blocking ASCT2 with V-9302 hydrochloride [1].
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| ln Vivo |
In both the HCT-116 and HT29 xenograft models, V-9302 hydrochloride (75 mg/kg; i.p.; once daily for 21 days) inhibits the growth of tumors [1]. SNU398 and MHCC97H cells produced as tumor xenografts in BALB/c nude mice; cultivated for 20 or 15 days, respectively) in combination with CB-839 and V-9302 hydrochloride (30 mg/kg; i.p.). caused a significant growth inhibition in transplantation models; however, the antitumor effects of a single medication therapy were only moderate [2]. Tumor growth was significantly reduced when V-9302 hydrochloride (50 mg/kg; i.p.; once daily for 5 days) was administered [3].
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| Animal Protocol |
Animal/Disease Models: 6-week old, female athymic nude mice (bearing HCT-116 (KRASG13D) or HT29 (BRAFV600E) cell-line)[1]
Doses: 75 mg/kg Route of Administration: intraperitoneally (ip); daily fo 21 days Experimental Results: Prevented tumor growth. |
| References |
[1]. Schulte ML, et al. Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacyin preclinical models. Nat Med. 2018 Feb;24(2):194-202.
[2]. Jin H, et al. A powerful drug combination strategy targeting glutamine addiction for the treatment of human liver cancer. Elife. 2020;9:e56749. Published 2020 Oct 5. [3]. Edwards DN, et al. Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer. J Clin Invest. 2021;131(4):e140100. |
| Molecular Formula |
C34H39CLN2O4
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|---|---|
| Molecular Weight |
575.14
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| CAS # |
2416138-42-4
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| Related CAS # |
V-9302;1855871-76-9
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 :~100 mg/mL (~173.87 mM )
H2O :~50 mg/mL (~86.94 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.62 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 (3.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7387 mL | 8.6935 mL | 17.3871 mL | |
| 5 mM | 0.3477 mL | 1.7387 mL | 3.4774 mL | |
| 10 mM | 0.1739 mL | 0.8694 mL | 1.7387 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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