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MedKoo Cat#: 563923 | Name: V-9302
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

V-9302 is a potent small-molecule antagonist of the glutamine transporter ASCT2 (SLC1A5) that inhibits glutamine uptake, leading to metabolic stress and suppression of tumor growth. In vitro studies have demonstrated that V-9302 effectively reduces glutamine consumption and downstream glutaminolysis, resulting in decreased ATP production, oxidative stress, and mTORC1 inhibition in cancer cells. It exhibits selective cytotoxicity against glutamine-addicted tumors, including triple-negative breast cancer, glioblastoma, and various other malignancies, while sparing non-transformed cells. Additionally, V-9302 has been shown to enhance the efficacy of metabolic stressors and chemotherapy agents, making it a promising candidate for combinational cancer therapy.

Chemical Structure

V-9302
V-9302
CAS#1855871-76-9 (free base)

Theoretical Analysis

MedKoo Cat#: 563923

Name: V-9302

CAS#: 1855871-76-9 (free base)

Chemical Formula: C34H38N2O4

Exact Mass: 538.2832

Molecular Weight: 538.69

Elemental Analysis: C, 75.81; H, 7.11; N, 5.20; O, 11.88

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to Ship
500mg USD 2,650.00 Ready to ship
1g USD 3,850.00 Ready to ship
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Related CAS #
1855871-76-9 (free base) 2416138-42-4 (HCl)
Synonym
V-9302; V9302; V 9302
IUPAC/Chemical Name
(S)-2-Amino-4-(bis(2-((3-methylbenzyl)oxy)benzyl)amino)butanoic acid
InChi Key
YGKNVAAMULVFNN-HKBQPEDESA-N
InChi Code
InChI=1S/C34H38N2O4/c1-25-9-7-11-27(19-25)23-39-32-15-5-3-13-29(32)21-36(18-17-31(35)34(37)38)22-30-14-4-6-16-33(30)40-24-28-12-8-10-26(2)20-28/h3-16,19-20,31H,17-18,21-24,35H2,1-2H3,(H,37,38)/t31-/m0/s1
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
May 7, 2024- Product V-9302 Patent licensing News MedKoo is excited to announce the licensing of patents of the novel compound V-9302 from Vanderbilt University. V-9302, a breakthrough compound, is now featured on our website at https://www.medkoo.com/products/28980 . V-9302 is a competitive antagonist of transmembrane glutamine flux (ASCT2 inhibitor), selectively and potently targeting the amino acid transporter ASCT2. This groundbreaking product is safeguarded by patents including US Patent US 10,793,514.
Biological target:
V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) with IC50=9.6 µM) in HEK-293 cells.
In vitro activity:
In the primary screen, this study observed that V-9302 exposure reduced in vitro viability by at least 20% in more than half of the cell lines screened, with sensitivity to V-9302 exposure not obviously linked to select mutational status (Extended Data Fig. 3). Follow-up screening was carried out in a subset of colorectal cancer (CRC) cell lines that exhibited variable sensitivities to V-9302 in the primary screen. Using three independent assays lacking ATP-dependency, this study confirmed that V-9302 exposure led to reduced cellular viability and increased cell death (Extended Data Fig. 4). Reference: Nat Med. 2018 Feb; 24(2): 194–202. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5803339/
In vivo activity:
To test the impact of glutamine uptake inhibition with V-9302, orthotopic E0771 tumors grown in immune-competent C57BL/6 female mice were treated daily with V-9302 (50 mg/kg) or vehicle beginning when tumors reached 100 mm3, equivalent to 11 days after tumor cell inoculation. Tumors treated with V-9302 displayed markedly reduced tumor growth (Figure 5A), resulting in decreased tumor weight upon collection on day 16, after only 5 days of treatment (Figure 5B). While V-9302 had only a marginal impact on Ki67+ cell proliferation, there was a more significant (3-fold) increase in apoptosis, as measured by cleaved caspase-3 (Figure 5C), in agreement with the increased cell death seen upon genetic GLS loss in E0771 tumors. Reference: J Clin Invest. 2021 Feb 15; 131(4): e140100. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7880417/
Solvent mg/mL mM
Solubility
DMSO 85.0 157.79
DMSO:PBS (pH 7.2) (1:2) 0.3 0.61
DMF 25.0 46.41
Ethanol 60.0 111.38
Water 50.5 93.75
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 538.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Park HY, Kim MJ, Kim YJ, Lee S, Jin J, Lee S, Choi YK, Park KG. V-9302 inhibits proliferation and migration of VSMCs, and reduces neointima formation in mice after carotid artery ligation. Biochem Biophys Res Commun. 2021 Jun 30;560:45-51. doi: 10.1016/j.bbrc.2021.04.079. Epub 2021 May 6. PMID: 33965788. 2. Schulte ML, Fu A, Zhao P, Li J, Geng L, Smith ST, Kondo J, Coffey RJ, Johnson MO, Rathmell JC, Sharick JT, Skala MC, Smith JA, Berlin J, Washington MK, Nickels ML, Manning HC. 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. 3. Edwards DN, Ngwa VM, Raybuck AL, Wang S, Hwang Y, Kim LC, Cho SH, Paik Y, Wang Q, Zhang S, Manning HC, Rathmell JC, Cook RS, Boothby MR, Chen J. Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer. J Clin Invest. 2021 Feb 15;131(4):e140100. doi: 10.1172/JCI140100. PMID: 33320840; PMCID: PMC7880417. 4. Schulte ML, Fu A, Zhao P, Li J, Geng L, Smith ST, Kondo J, Coffey RJ, Johnson MO, Rathmell JC, Sharick JT, Skala MC, Smith JA, Berlin J, Washington MK, Nickels ML, Manning HC. 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.
In vitro protocol:
1. Park HY, Kim MJ, Kim YJ, Lee S, Jin J, Lee S, Choi YK, Park KG. V-9302 inhibits proliferation and migration of VSMCs, and reduces neointima formation in mice after carotid artery ligation. Biochem Biophys Res Commun. 2021 Jun 30;560:45-51. doi: 10.1016/j.bbrc.2021.04.079. Epub 2021 May 6. PMID: 33965788. 2. Schulte ML, Fu A, Zhao P, Li J, Geng L, Smith ST, Kondo J, Coffey RJ, Johnson MO, Rathmell JC, Sharick JT, Skala MC, Smith JA, Berlin J, Washington MK, Nickels ML, Manning HC. 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.
In vivo protocol:
1. Edwards DN, Ngwa VM, Raybuck AL, Wang S, Hwang Y, Kim LC, Cho SH, Paik Y, Wang Q, Zhang S, Manning HC, Rathmell JC, Cook RS, Boothby MR, Chen J. Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer. J Clin Invest. 2021 Feb 15;131(4):e140100. doi: 10.1172/JCI140100. PMID: 33320840; PMCID: PMC7880417. 2. Schulte ML, Fu A, Zhao P, Li J, Geng L, Smith ST, Kondo J, Coffey RJ, Johnson MO, Rathmell JC, Sharick JT, Skala MC, Smith JA, Berlin J, Washington MK, Nickels ML, Manning HC. 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.
1: Jiang Q, Lu S, Xu X, Bai C, Yan Q, Fang M, Huang L, Jin C, Zhang Y, Sun J, He Z, Zhao C, Qin F, Wang Y, Zhang T. Corrigendum to "Inhibition of alanine-serine- cysteine transporter 2-mediated auto-enhanced photodynamic cancer therapy of co- nanoassembly between V-9302 and photosensitizer" [J. Colloid Interface Sci. 629 (2023) 773-784]. J Colloid Interface Sci. 2025 Jan 15;678(Pt B):1025. doi: 10.1016/j.jcis.2024.08.242. Epub 2024 Sep 13. Erratum for: J Colloid Interface Sci. 2023 Jan;629(Pt B):773-784. doi: 10.1016/j.jcis.2022.05.044. PMID: 39276511. 2: Ren H, Wu Z, Tan J, Tao H, Zou W, Cao Z, Wen B, Cai Z, Du J, Deng Z. Co- delivery Nano System of MS-275 and V-9302 Induces Pyroptosis and Enhances Anti- Tumor Immunity Against Uveal Melanoma. Adv Sci (Weinh). 2024 Aug;11(31):e2404375. doi: 10.1002/advs.202404375. Epub 2024 Jun 18. PMID: 38889339; PMCID: PMC11336933. 3: Yang R, Zhang S, Wang L, Chen Y, Chen X, Xia J, Ren X, Cheng B, Chen X. Radiation-induced exosomes promote oral squamous cell carcinoma progression via enhancing SLC1A5-glutamine metabolism. J Oral Pathol Med. 2024 Aug;53(7):458-467. doi: 10.1111/jop.13561. Epub 2024 May 27. PMID: 38802300. 4: Wang X, Ding B, Liu W, Qi L, Li J, Zheng X, Song Y, Li Q, Wu J, Zhang M, Chen H, Wang Y, Li Y, Sun B, Ma P. Dual Starvations Induce Pyroptosis for Orthotopic Pancreatic Cancer Therapy through Simultaneous Deprivation of Glucose and Glutamine. J Am Chem Soc. 2024 Jul 3;146(26):17854-17865. doi: 10.1021/jacs.4c03478. Epub 2024 May 22. PMID: 38776361. 5: Taurino G, Dander E, Chiu M, Pozzi G, Maccari C, Starace R, Silvestri D, Griffini E, Bianchi MG, Carubbi C, Andreoli R, Mirandola P, Valsecchi MG, Rizzari C, D'Amico G, Bussolati O. Asparagine transport through SLC1A5/ASCT2 and SLC38A5/SNAT5 is essential for BCP-ALL cell survival and a potential therapeutic target. Br J Haematol. 2024 Jul;205(1):175-188. doi: 10.1111/bjh.19516. Epub 2024 May 13. PMID: 38736325. 6: Ahn SH, Jang SK, Kim MJ, Kim G, Park KS, Hong J, Lee TG, Kim CH, Park IC, Jin HO. Downregulation of TRIB3 enhances the sensitivity of lung cancer cells to amino acid deprivation by suppressing AKT activation. Am J Cancer Res. 2024 Apr 15;14(4):1622-1633. doi: 10.62347/GLSY2976. PMID: 38726284; PMCID: PMC11076249. 7: Fu X, Wu H, Li C, Deng G, Chen C. YAP1 inhibits RSL3-induced castration- resistant prostate cancer cell ferroptosis by driving glutamine uptake and metabolism to GSH. Mol Cell Biochem. 2024 Sep;479(9):2415-2427. doi: 10.1007/s11010-023-04847-4. Epub 2023 Sep 29. PMID: 37773303; PMCID: PMC11371892. 8: Choudhury M, Schaefbauer KJ, Kottom TJ, Yi ES, Tschumperlin DJ, Limper AH. Targeting Pulmonary Fibrosis by SLC1A5-Dependent Glutamine Transport Blockade. Am J Respir Cell Mol Biol. 2023 Oct;69(4):441-455. doi: 10.1165/rcmb.2022-0339OC. PMID: 37459644; PMCID: PMC10557918. 9: Sbirkov Y, Vergov B, Dzharov V, Schenk T, Petrie K, Sarafian V. Targeting Glutaminolysis Shows Efficacy in Both Prednisolone-Sensitive and in Metabolically Rewired Prednisolone-Resistant B-Cell Childhood Acute Lymphoblastic Leukaemia Cells. Int J Mol Sci. 2023 Feb 8;24(4):3378. doi: 10.3390/ijms24043378. PMID: 36834787; PMCID: PMC9965631. 10: Adhikary G, Shrestha S, Naselsky W, Newland JJ, Chen X, Xu W, Emadi A, Friedberg JS, Eckert RL. Mesothelioma cancer cells are glutamine addicted and glutamine restriction reduces YAP1 signaling to attenuate tumor formation. Mol Carcinog. 2023 Apr;62(4):438-449. doi: 10.1002/mc.23497. Epub 2022 Dec 23. PMID: 36562471; PMCID: PMC10071591. 11: Jiang Q, Lu S, Xu X, Bai C, Yan Q, Fang M, Huang L, Jin C, Zhang Y, Sun J, He Z, Zhao C, Qin F, Wang Y, Zhang T. Inhibition of alanine-serine-cysteine transporter 2-mediated auto-enhanced photodynamic cancer therapy of co- nanoassembly between V-9302 and photosensitizer. J Colloid Interface Sci. 2023 Jan;629(Pt B):773-784. doi: 10.1016/j.jcis.2022.05.044. Epub 2022 May 27. Erratum in: J Colloid Interface Sci. 2025 Jan 15;678(Pt B):1025. doi: 10.1016/j.jcis.2024.08.242. PMID: 36195017. 12: Kim G, Jang SK, Kim YJ, Jin HO, Bae S, Hong J, Park IC, Lee JH. Inhibition of Glutamine Uptake Resensitizes Paclitaxel Resistance in SKOV3-TR Ovarian Cancer Cell via mTORC1/S6K Signaling Pathway. Int J Mol Sci. 2022 Aug 6;23(15):8761. doi: 10.3390/ijms23158761. PMID: 35955892; PMCID: PMC9369036. 13: Pollard AC, Paolillo V, Radaram B, Qureshy S, Li L, Maity T, Wang L, Uddin MN, Wood CG, Karam JA, Pagel MD, Piwnica-Worms D, Millward SW, Fowlkes NW, Norton W, Engel BJ, Pisaneschi F, Zacharias NM. PET/MR Imaging of a Lung Metastasis Model of Clear Cell Renal Cell Carcinoma with (2S,4R)-4-[18F]Fluoroglutamine. Mol Imaging Biol. 2022 Dec;24(6):959-972. doi: 10.1007/s11307-022-01747-9. Epub 2022 Jun 22. PMID: 35732988; PMCID: PMC9681699. 14: Zhou Q, Lin W, Wang C, Sun F, Ju S, Chen Q, Wang Y, Chen Y, Li H, Wang L, Hu Z, Jin H, Wang X, Sun Y. Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells. Nat Commun. 2022 May 31;13(1):3034. doi: 10.1038/s41467-022-30559-2. Erratum in: Nat Commun. 2022 Jun 14;13(1):3424. doi: 10.1038/s41467-022-31203-9. PMID: 35641493; PMCID: PMC9156729. 15: Li QQ, Pan SY, Chen QY, Zhou W, Wang SQ. [Effect of Competitive Antagonist of Transmembrane Glutamine Flux V-9302 on Apoptosis of Acute Myeloid Leukemia Cell Lines HL-60 and KG-1]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2021 Jun;29(3):685-689. Chinese. doi: 10.19746/j.cnki.issn.1009-2137.2021.03.005. PMID: 34105457. 16: Park HY, Kim MJ, Kim YJ, Lee S, Jin J, Lee S, Choi YK, Park KG. V-9302 inhibits proliferation and migration of VSMCs, and reduces neointima formation in mice after carotid artery ligation. Biochem Biophys Res Commun. 2021 Jun 30;560:45-51. doi: 10.1016/j.bbrc.2021.04.079. Epub 2021 May 6. PMID: 33965788. 17: Edwards DN, Ngwa VM, Raybuck AL, Wang S, Hwang Y, Kim LC, Cho SH, Paik Y, Wang Q, Zhang S, Manning HC, Rathmell JC, Cook RS, Boothby MR, Chen J. Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer. J Clin Invest. 2021 Feb 15;131(4):e140100. doi: 10.1172/JCI140100. PMID: 33320840; PMCID: PMC7880417. 18: Jin H, Wang S, Zaal EA, Wang C, Wu H, Bosma A, Jochems F, Isima N, Jin G, Lieftink C, Beijersbergen R, Berkers CR, Qin W, Bernards R. A powerful drug combination strategy targeting glutamine addiction for the treatment of human liver cancer. Elife. 2020 Oct 5;9:e56749. doi: 10.7554/eLife.56749. PMID: 33016874; PMCID: PMC7535927. 19: Baguet T, Bouton J, Janssens J, Pauwelyn G, Verhoeven J, Descamps B, Van Calenbergh S, Vanhove C, De Vos F. Radiosynthesis, in vitro and preliminary biological evaluation of [18 F]2-amino-4-((2-((3-fluorobenzyl)oxy)ben zyl)(2-((3-(fluoromethyl)benzyl)oxy)benzyl)amino)butanoic acid, a novel alanine serine cysteine transporter 2 inhibitor-based positron emission tomography tracer. J Labelled Comp Radiopharm. 2020 Aug;63(10):442-455. doi: 10.1002/jlcr.3863. Epub 2020 Jul 6. PMID: 32472945. 20: Jiang H, Zhang N, Tang T, Feng F, Sun H, Qu W. Target the human Alanine/Serine/Cysteine Transporter 2(ASCT2): Achievement and Future for Novel Cancer Therapy. Pharmacol Res. 2020 Aug;158:104844. doi: 10.1016/j.phrs.2020.104844. Epub 2020 May 11. PMID: 32438035.