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Chemical Structure| 1855871-76-9 Chemical Structure| 1855871-76-9

Structure of V-9302
CAS No.: 1855871-76-9

Chemical Structure| 1855871-76-9

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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.

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Product Details of V-9302

CAS No. :1855871-76-9
Formula : C34H38N2O4
M.W : 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

Safety of V-9302

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of V-9302

ferroptosis

Isoform Comparison

Biological Activity

In Vitro:

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

In Vivo:

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

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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