V-9302 是跨膜谷氨酰胺通量的竞争性拮抗剂。V-9302 有效选择性的靶向氨基酸转运体ASCT2 (SLC1A5),不是 ASCT1。V-9302 抑制了 HEK-293 细胞中由 ASCT2 介导的谷氨酰胺摄取 (IC50=9.6 μM)。
生物活性 | V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporterASCT2 (SLC1A5)not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells[1]. |
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体外研究 (In Vitro) | V-9302 inhibits ASCT2-mediated glutamine uptake in human cells in a concentration-dependent fashion and exhibits a 100-fold improvement in potency over gamma-L-glutamyl-p-nitroanilide[1]. Pharmacological blockade of ASCT2 with V-9302 results in attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress[1].
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体内研究 (In Vivo) | V-9302 (75 mg/kg; i.p.; daily fo 21 days) prevents tumor growth in both HCT-116 and HT29 xenograft models[1]. The combination of CB-839 and V-9302 (30 mg/kg; i.p.; SNU398 and MHCC97H cells were grown as tumor xenografts in BALB/c nude mice; for 20 or 15 d, respectively) elicits a strong growth inhibition in both SNU398 and MHCC97H xenograft models, while single-drug treatment showed modest anti-tumor effects[2]. V-9302 (50 mg/kg ; i.p.; daily for 5 days) displays markedly reduced tumor growth[3].
Animal Model: | 6-week old, female athymic nude mice (bearing HCT-116 (KRAS G13D) or HT29 (BRAF V600E) cell-line)[1] | Dosage: | 75 mg/kg | Administration: | Intraperitoneally; daily fo 21 days | Result: | Prevented tumor growth. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 25 mg/mL(46.41 mM;ultrasonic and warming and heat to 80℃) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 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 |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1 mg/mL (1.86 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (1.86 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 1 mg/mL (1.86 mM); Suspended solution; Need ultrasonic
此方案可获得 1 mg/mL (1.86 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1 mg/mL (1.86 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (1.86 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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