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V-9302 {[allProObj[0].p_purity_real_show]}

货号:A1002473

V-9302是一种竞争性且选择性的跨膜谷氨酰胺流通抑制剂,选择性且高效地靶向氨基酸转运蛋白 ASCT2,IC50 为 9.6 μM。

V-9302 化学结构 CAS号:1855871-76-9
V-9302 化学结构
CAS号:1855871-76-9
V-9302 3D分子结构
CAS号:1855871-76-9
V-9302 化学结构 CAS号:1855871-76-9
V-9302 3D分子结构 CAS号:1855871-76-9
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V-9302 纯度/质量文件 产品仅供科研

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V-9302 生物活性

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.

V-9302 细胞实验

Cell Line
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

V-9302 动物实验

Species
Animal Model
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

V-9302 实验方案

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

V-9302 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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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