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| 描述 | V-9302 is a competitive and selective antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 with IC50 of 9.6 μM. |
| Concentration | Treated Time | Description | References | |
| HEK293 cells | 50 µM | 1 hour | Inhibition of ASCT2-mediated glutamine transport, reducing [18F]FGln uptake by 20-50% | Mol Imaging Biol. 2022 Dec;24(6):959-972. |
| UMRC3 cells | 50 µM | 1 hour | Inhibition of ASCT2-mediated glutamine transport, reducing [18F]FGln uptake by 20-50% | Mol Imaging Biol. 2022 Dec;24(6):959-972. |
| H1299 lung cancer cells | 20 µM | 12 hours | To evaluate the effect of V-9302 on H1299 cells, results showed that V-9302 increased ATF4 and TRIB3 mRNA levels and elevated p-AKT Ser473 protein levels. | Am J Cancer Res. 2024 Apr 15;14(4):1622-1633. |
| HEK-293 cells | 9.6 µM (IC 50) | 15 minutes | Evaluate the inhibitory effect of V-9302 on ASCT2-mediated glutamine uptake | Nat Med. 2018 Feb;24(2):194-202. |
| H1299 lung cancer cells | 20 µM | 24 hours | To evaluate the effect of V-9302 on H1299 cells, results showed that TRIB3 knockdown enhanced the V-9302-induced decrease in cell viability. | Am J Cancer Res. 2024 Apr 15;14(4):1622-1633. |
| 92.1 | 2 µM | 24 hours | Evaluate the cytotoxicity of V-9302 in combination with MS-275, showing that the combination treatment significantly outperformed single treatments. | Adv Sci (Weinh). 2024 Aug;11(31):e2404375. |
| MUM-2B | 2 µM | 24 hours | Evaluate the cytotoxicity of V-9302 in combination with MS-275, showing that the combination treatment significantly outperformed single treatments. | Adv Sci (Weinh). 2024 Aug;11(31):e2404375. |
| OCM-1 | 2 µM | 24 hours | Evaluate the cytotoxicity of V-9302 in combination with MS-275, showing that the combination treatment significantly outperformed single treatments. | Adv Sci (Weinh). 2024 Aug;11(31):e2404375. |
| AKR-2B cells | 10 µM | 24 hours | To evaluate the effect of V-9302 on cell migration. Results showed V-9302 significantly inhibited TGF-β-stimulated cell migration. | Am J Respir Cell Mol Biol. 2023 Oct;69(4):441-455. |
| NCI-Meso-17 cells | 15 µM | 24 hours | Inhibits SLC1A5-dependent glutamine uptake, significantly reducing mesothelioma cell proliferation, spheroid formation, and invasion | Mol Carcinog. 2023 Apr;62(4):438-449. |
| Meso-1 cells | 15 µM | 24 hours | Inhibits SLC1A5-dependent glutamine uptake, significantly reducing mesothelioma cell proliferation, spheroid formation, and invasion | Mol Carcinog. 2023 Apr;62(4):438-449. |
| DU145 cells | 20 µM | 48 hours | Inhibited SLC1A5 activity, reduced GSH levels and GPX4 activity, increased ROS and MDA levels, and promoted ferroptosis in CRPC cells | Mol Cell Biochem. 2024 Sep;479(9):2415-2427. |
| PC-3 cells | 20 µM | 48 hours | Inhibited SLC1A5 activity, reduced GSH levels and GPX4 activity, increased ROS and MDA levels, and promoted ferroptosis in CRPC cells | Mol Cell Biochem. 2024 Sep;479(9):2415-2427. |
| HT29 cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on pS6 and pERK levels, showing decreased pS6 and pERK levels | Nat Med. 2018 Feb;24(2):194-202. |
| HCC1806 cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on cell growth and proliferation, showing increased cell death and oxidative stress | Nat Med. 2018 Feb;24(2):194-202. |
| FaDu cells | 25 µM | 48 hours | To evaluate the effect of V-9302 on glutamine uptake in ASCT2-silenced FaDu cells, results showed that V-9302 significantly reduced glutamine uptake. | Br J Cancer. 2020 Jan;122(1):82-93. |
| SCC15 cells | 25 µM | 48 hours | To evaluate the effect of V-9302 on glutamine uptake in ASCT2-silenced SCC15 cells, results showed that V-9302 significantly reduced glutamine uptake. | Br J Cancer. 2020 Jan;122(1):82-93. |
| IPF fibroblasts | 10 µM | 48 hours | To evaluate the effect of V-9302 on profibrotic marker expression in IPF fibroblasts. Results showed V-9302 significantly inhibited the expression of Col1, FN, and ACTA2. | Am J Respir Cell Mol Biol. 2023 Oct;69(4):441-455. |
| Normal human lung fibroblasts (NHLFs) | 10 µM | 48 hours | To evaluate the effect of V-9302 on TGF-β-induced profibrotic molecule expression. Results showed V-9302 significantly inhibited the expression of Col1, CTGF, FN, and ACTA2. | Am J Respir Cell Mol Biol. 2023 Oct;69(4):441-455. |
| SKOV3-TR cells | 20 µM | 48 hours | Inhibited mTORC1/S6K signaling pathway, reduced cell viability | Int J Mol Sci. 2022 Aug 6;23(15):8761. |
| Breast cancer cells BT549 | 5 µM | 72 hours | V-9302 enhanced the sensitivity of breast cancer cells to MLN4924 and inhibited cell growth | Nat Commun. 2022 May 31;13(1):3034. |
| Breast cancer cells MDA-MB-231 | 5 µM | 72 hours | V-9302 enhanced the sensitivity of breast cancer cells to MLN4924 and inhibited cell growth | Nat Commun. 2022 May 31;13(1):3034. |
| HT29 cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on pERK and oxidative stress | Nat Med. 2018 Feb;24(2):194-202 |
| HCC1806 cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on pS6 and pERK | Nat Med. 2018 Feb;24(2):194-202 |
| HEK-293 cells | 9.6 µM | 15 minutes | Evaluate the inhibitory effect of V-9302 on ASCT2-mediated glutamine uptake | Nat Med. 2018 Feb;24(2):194-202 |
| RKO cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on cell viability | Nat Med. 2018 Feb;24(2):194-202 |
| HT29 cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on oxidative stress | Nat Med. 2018 Feb;24(2):194-202 |
| HCC1806 cells | 25 µM | 48 hours | Evaluate the effect of V-9302 on pS6 and pERK | Nat Med. 2018 Feb;24(2):194-202 |
| HEK-293 cells | 9.6 µM | 15 minutes | Evaluate the inhibitory effect of V-9302 on ASCT2-mediated glutamine uptake | Nat Med. 2018 Feb;24(2):194-202 |
| Administration | Dosage | Frequency | Description | References | ||
| NOD/scid/IL-2 receptor gamma chain knockout mice | Mesothelioma xenograft model | Intraperitoneal injection | 15 mg/kg | Three times per week for ten weeks | V-9302 treatment significantly inhibits mesothelioma tumor growth and reduces the expression of YAP1/TEAD signaling pathway-related proteins | Mol Carcinog. 2023 Apr;62(4):438-449. |
| Nude mice | MDA-MB-231 xenograft tumor model | Intraperitoneal injection | 20 mg/kg | 5 days a week for 14 days | V-9302 combined with MLN4924 significantly inhibited tumor growth | Nat Commun. 2022 May 31;13(1):3034. |
| BALB/c nude mice | SNU398 and MHCC97H xenograft models | Intraperitoneal injection | 30 mg/kg | 5 days per week for 15 or 20 days | The combination of V-9302 and CB-839 significantly inhibited tumor growth and induced apoptosis in vivo. | Elife. 2020 Oct 5;9:e56749 |
| C57BL/6 mice | Bleomycin-induced pulmonary fibrosis model | Intraperitoneal injection | 37.5 mg/kg/day | Daily for 13 days | To evaluate the therapeutic effect of V-9302 on bleomycin-induced pulmonary fibrosis. Results showed V-9302 significantly improved lung function, reduced collagen deposition, and decreased profibrotic marker expression. | Am J Respir Cell Mol Biol. 2023 Oct;69(4):441-455. |
| BALB/c nude mice | OCM-1 tumor model | Intravenous injection | 4 mg/kg | 16-day treatment cycle | Evaluate the anti-tumor efficacy of NPs in vivo, showing that NPs significantly inhibited tumor growth. | Adv Sci (Weinh). 2024 Aug;11(31):e2404375. |
| Mice | E0771 tumor model | Intraperitoneal injection | 50 mg/kg | Once daily for 5 days | Evaluate the effect of V-9302 on tumor growth and T cell activation | J Clin Invest. 2021 Feb 15;131(4):e140100 |
| Athymic nude mice | HCT-116 and HT29 cell-line xenograft models | Intraperitoneal injection | 75 mg/kg | Once daily for 21 days | Evaluate the inhibitory effect of V-9302 on tumor growth, showing suppressed tumor growth, decreased pS6 levels, and increased cleaved caspase 3 levels | Nat Med. 2018 Feb;24(2):194-202. |
| Nude mice | HNSCC xenograft model | Intraperitoneal injection | 75 mg/kg | Once daily for 35 days | To evaluate the effect of V-9302 on the growth of ASCT2-silenced HNSCC xenografts, results showed that V-9302 significantly inhibited tumor growth. | Br J Cancer. 2020 Jan;122(1):82-93. |
| Nude mice | HCT-116 and HT29 cell-line xenograft models | Intraperitoneal injection | 75 mg/kg | Once daily for 21 days | Evaluate the inhibitory effect of V-9302 on tumor growth | Nat Med. 2018 Feb;24(2):194-202 |
| Nude mice | Liver cancer xenograft model | Intraperitoneal injection | 75 mg/kg/day | Once daily for 15 days | To investigate the effect of targeting Rictor/mTORC2-HDAC3/GS axis on glutamine starvation-induced liver TICs, results showed that inhibiting Rictor/mTORC2-HDAC3/GS axis could inhibit TICs and promote tumor regression | Adv Sci (Weinh). 2022 Jul;9(20):e2103887 |
| Nude mice | HCT-116 and HT29 cell-line xenograft models | Intraperitoneal injection | 75 mg/kg | Once daily for 21 days | Evaluate the inhibitory effect of V-9302 on tumor growth | Nat Med. 2018 Feb;24(2):194-202 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.86mL 0.37mL 0.19mL |
9.28mL 1.86mL 0.93mL |
18.56mL 3.71mL 1.86mL |
|
| CAS号 | 1855871-76-9 |
| 分子式 | C34H38N2O4 |
| 分子量 | 538.68 |
| SMILES Code | O=C(O)[C@@H](N)CCN(CC1=CC=CC=C1OCC2=CC=CC(C)=C2)CC3=CC=CC=C3OCC4=CC=CC(C)=C4 |
| MDL No. | MFCD32062750 |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 25 mg/mL(46.41 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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