WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H563923
CAS#: 1855871-76-9
Description: V-9302 is a competitive antagonist of transmembrane glutamine flux (ASCT2 inhibitor), selectively and potently targeting the amino acid transporter ASCT2.
Hodoodo Cat#: H563923
Name: V-9302
CAS#: 1855871-76-9
Chemical Formula: C34H38N2O4
Exact Mass: 538.28
Molecular Weight: 538.690
Elemental Analysis: C, 75.81; H, 7.11; N, 5.20; O, 11.88
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:
| 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 | Max Conc. mg/mL | Max Conc. 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 |
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.
| 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: 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. PubMed PMID: 29334372; PubMed Central PMCID: PMC5803339.
