V-9302
目录号 : GC34852
An inhibitor of ASCT2
Cas No.:1855871-76-9
Sample solution is provided at 25 µL, 10mM.
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V-9302 is an inhibitor of amino acid transporter 2 (ASCT2).1 It inhibits glutamine uptake with IC50 values of 9 and 9.6 ?M for the rat and human transporters, respectively. V-9302 also inhibits glutamine uptake in HEK293 cells and reduces cell viability of a variety of cancer cell lines, including HCT116, HT-29, COLO 205, and RKO cells (EC50s = 8.9, 9.4, 14.5, and 8.3 ?M, respectively).2 It reduces glutamine uptake into tumor tissue and prevents tumor growth in HCT116 and HT-29 mouse xenograft models expressing K-RasG13D and BRAFV600E mutations, respectively, when administered at a dose of 75 mg/kg per day for 21 days.
1.Schulte, M.L., Khodadadi, A.B., Cuthbertson, M.L., et al.2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transportBioorg. Med. Chem. Lett.26(3)1044-1047(2016) 2.Schulte, M.L., Fu, A., Zhao, P., et al.Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical modelsNat. Med.24(2)194-202(2018)
| Cell experiment [1]: | |
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Cell lines |
HCC1806 cells |
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Preparation Method |
Cells were plated in 96-well plates for 24 h before the assay. Cells were treated with either vehicle or the indicated concentrations（25 μM） of V-9302 hydrochloride for 48 h |
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Reaction Conditions |
25 μM，48h |
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Applications |
Silencing of ASCT2 and V-9302 hydrochloride exposure in HCC1806 cells resulted in analogous downstream effects, including markedly decreased phosphorylated (p)-S6 levels and a modest decrease in p-ERK levels. |
| Animal experiment [2]: | |
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Animal models |
6-week-old female athymic nude mice |
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Preparation Method |
Chronic-exposure studies in tumor-bearing mice. Athymic nude mice (Hsd:Athymic nude-Foxn1nu) bearing HCT-116 (KRAS-G13D) or HT29 (BRAF-V600E) cell line xenografts were treated with 75 mg V-9302 hydrochloride per kg body weight per day for 21 d. |
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Dosage form |
75 mg V-9302 hydrochloride per kg body weight per day for 21 day |
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Applications |
V-9302 hydrochloride led to significantly decreased expression of p-S6 in tumor tissue in both HCT-116 and HT29 xenografts. In addition to decreased p-S6 IHC staining, V-9302 treatment led to elevated levels of cleaved caspase 3 in both HCT-116 and HT29 xenografts. |
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References: [1]. Schulte ML, Fu A, et,al. Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical models. Nat Med. 2018 Feb;24(2):194-202. doi: 10.1038/nm.4464. Epub 2018 Jan 15. PMID: 29334372; PMCID: PMC5803339. |
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| Cas No. | 1855871-76-9 | SDF | |
| Canonical SMILES | O=C(O)[C@@H](N)CCN(CC1=CC=CC=C1OCC2=CC=CC(C)=C2)CC3=CC=CC=C3OCC4=CC=CC(C)=C4 | ||
| 分子式 | C34H38N2O4 | 分子量 | 538.68 |
| 溶解度 | DMSO : 125 mg/mL (232.05 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8564 mL | 9.2819 mL | 18.5639 mL |
| 5 mM | 0.3713 mL | 1.8564 mL | 3.7128 mL |
| 10 mM | 0.1856 mL | 0.9282 mL | 1.8564 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet